Publications & Patents

456. The Art and Science of Total Synthesis at the Dawn of the Twenty-First Century, K.C. Nicolaou, D. Vourloumis, N. Winssinger, P.S. Baran, Angew. Chem. Int. Ed. 2000, 39, 44–122.

457. Solid-Phase Combinatorial Synthesis Using MicroKan Reactors, Rf Tagging, and Directed Sorting, X.-Y. Xiao, R. Li, H. Zhuang, B. Ewing, K. Karunaratne, J. Lillig, R. Brown, K.C. Nicolaou, Biotechnol. Bioengin. (Combinatorial Chemistry) 2000, 71, 44–50.

458. New Synthetic Technology for the Rapid Construction of Novel Heterocycles. 1. The Reaction of Dess–Martin Periodinane with Anilides and Related Compounds, K.C. Nicolaou, Y.-L. Zhong, P.S. Baran, Angew. Chem. Int. Ed. 2000, 39, 622–625.

459. New Synthetic Technology for the Rapid Construction of Novel Heterocycles. 2. The Reaction of IBX with Anilides and Related Compounds, K.C. Nicolaou, Y.-L. Zhong, P.S. Baran, Angew. Chem. Int. Ed. 2000, 39, 625–628.

460. Selenium-Based Solid-Phase Synthesis of Benzopyrans I: Applications to Combinatorial Synthesis of Natural Products, K.C. Nicolaou, J.A. Pfefferkorn, G.-Q. Cao, Angew. Chem. Int. Ed. 2000, 39, 734–739.

461. Selenium-Based Solid-Phase Synthesis of Benzopyrans II: Applications to Combinatorial Synthesis of Medicinally Relevant Small Organic Molecules, K.C. Nicolaou, J.A. Pfefferkorn, G.-Q. Cao, Angew. Chem. Int. Ed. 2000, 39, 739–743.

462. Synthesis of the Macrocyclic Core of Apoptolidin, K.C. Nicolaou, Y. Li, B. Weyerhausen, H. Wei, Chem. Commun. 2000, 307–308.

463. New Selenium-Based Safety-Catch Linkers.  Solid-Phase Semisynthesis of Vancomycin, K.C. Nicolaou, N. Winssinger, R. Hughes, C. Smethurst, S.Y. Cho, Angew. Chem. Int. Ed. 2000, 39, 1084–1088.

464. 1,2-Seleno Migrations in Carbohydrate Chemistry: Solution and Solid-Phase Synthesis of 2-Deoxy Glycosides, Orthoesters, and Allyl Orthoesters, K.C. Nicolaou, H.J. Mitchell, K.C. Fylaktakidou, H. Suzuki, R. Rodriguez, Angew. Chem. Int. Ed. 2000, 39, 1089–1093.

465. Solution and Solid-Phase Synthesis of Functionalized 3-Arylbenzofurans by a Novel Cyclofragmentation - Release Pathway, K.C. Nicolaou, S.A Snyder, A. Bigot, J. Pfefferkorn, Angew. Chem. Int. Ed. 2000, 39, 1093–1096.

466. A Common Pharmacophore for Epothilones and Taxol: Molecular Basis for Drug Resistance-Conferred by Tubulin Mutations in Human Cancer Cells, P. Giannakakou, R. Gussio, E. Nogales, K.H. Downing, D. Zaharevitz, B. Bollbuck, G. Poy, D. Sackett, K.C. Nicolaou, T. Fojo, Proc. Natl. Acad. Sci. USA 2000, 97, 2904–2909.

467. A Novel Strategy for the Solid Phase Synthesis of Substituted Indolines, K.C. Nicolaou, A.J. Roecker, J.A. Pfefferkorn, G.-Q. Cao, J. Am. Chem. Soc. 2000, 122, 2966–2967.

468. Biomimetic Total Synthesis of Bisorbicillinol, Bisorbitutenolide, Trichodimerol, and Designed Analogues of the Bisorbicillinoids, K.C. Nicolaou, G. Vassilikogiannakis, K.B. Simonsen, P.S. Baran, Y.-L. Zhong, V.P. Vidali, E.N. Pitsinos, E.A. Couladouros, J. Am. Chem. Soc. 2000, 122, 3071–3079.

469. Total Synthesis of the Immunosuppressant Sanglifehrin A, K.C. Nicolaou, F. Murphy, S. Barluenga, T. Ohshima, H.Wei, J. Xu, D.L.F. Gray, O. Baudoin, J. Am. Chem. Soc. 2000, 122, 3830–3838.

470. The Absolute Configuration and Asymmetric Total Synthesis of the CP Molecules (CP-263,114 and CP-225,917, Phomoidrides B and A), K.C. Nicolaou, J.-K. Jung, W.H. Yoon, Y. He, Y.-L. Zhong, P.S. Baran, Angew. Chem. Int. Ed. 2000, 39, 1829–1832.

471. New Synthetic Technology for the Mild and Selective One-Carbon Homologation of Hindered Aldehydes in the Presence of Ketones, K.C. Nicolaou, G. Vassilikogiannakis, R. Kranich, P.S. Baran, Y.-L. Zhong, S. Natarajan, Org. Lett. 2000, 2, 1895–1898.

472. High Throughput Combinatorial Synthesis of Discrete Compounds in Multimilligram Quantity: Non-chemical Encoding and Directed Sorting, X.-Y. Xiao, K.C. Nicolaou, in Combinatorial Chemistry- A Practical Approach, Hicham Fenniri, Ed., Oxford University Press, New York, 2000, pp. 75–93.

473. Novel IBX-Mediated Processes for the Synthesis of Amino Sugars and Libraries Thereof, K.C. Nicolaou, P.S. Baran, Y.-L. Zhong, J.A. Vega, Angew. Chem. Int. Ed. 2000, 39, 2525–2529.

474. Novel Reactions Initiated by Titanocene Methylidenes: Deoxygenation of Sulfoxides, N–Oxides, and Selenoxides, K.C. Nicolaou, A.E. Koumbis, S.A. Snyder, K.B. Simonsen, Angew. Chem. Int. Ed. 2000, 39, 2529–2533.

475. Total Synthesis of 16-Desmethylepothilone B, Epothilone B10, Epothilone F, and Related Side Chain Modified Epothilone B Analogues, K.C. Nicolaou, D. Hepworth, N.P. King, M.R.V. Finlay, R. Scarpelli, M.M.A. Pereira, B. Bollbuck, A. Bigot, B. Werschkun, N. Winssinger, Chem. Eur. J. 2000, 6, 2783–2800.

476. A New Method for the One-Step Synthesis of α, β-Unsaturated Carbonyl Systems from Saturated Alcohols and Carbonyl Compounds, K.C. Nicolaou, Y.-L. Zhong, P.S. Baran, J. Am. Chem. Soc. 2000, 122, 7596–7597.

477. Chemical Synthesis and Biological Properties of Pyridine Epothilones, K.C. Nicolaou, R. Scarpelli, B. Bollbuck, B. Werschkun, M.M.A. Pereira, M. Wartmann, K.-H. Altmann, D. Zaharevitz, R. Gussio, P. Giannakakou, Chem. Biol. 2000, 7, 593–599.

478. Total Synthesis of Everninomicin 13,384-1. Part 1: Retrosynthetic Analysis and Synthesis of the A1B(A)C Fragment, K.C. Nicolaou, R.M. Rodríguez, H.J. Mitchell, H. Suzuki, K.C. Fylaktakidou, O. Baudoin, F.L. van Delft, Chem. Eur. J. 2000, 6, 3095–3115.

479. Total Synthesis of Everninomicin 13,384-1. Part 2: Synthesis of the FGHA2 Fragment, K. C. Nicolaou, H.J. Mitchell, K.C. Fylaktakidou, R.M. Rodríguez, H. Suzuki, Chem. Eur. J. 2000, 6, 3116–3148.

480. Total Synthesis of Everninomicin 13,384-1. Part 3: Synthesis of the DE Fragment and Completion of the Total Synthesis, K.C. Nicolaou, H.J. Mitchell, R.M. Rodríguez, K.C. Fylaktakidou, H. Suzuki, S.R. Conley, Chem. Eur. J. 2000, 6, 3149–3165.

481. Total Synthesis of Everninomicin 13,384-1. Part 4: Explorations of Methodology. Stereocontrolled Synthesis of 1,1'-Disaccharides, 1,2-Seleno Migrations in Carbohydrates, and Solution and Solid Phase Synthesis of 2-Deoxy Glycosides and Orthoesters, K.C. Nicolaou, K.C. Fylaktakidou, H.J. Mitchell, F.L. van Delft, R.M. Rodríguez, S.R. Conley, Z. Jin, Chem. Eur. J. 2000, 6, 3166–3185.

482. Total Synthesis and Biological Evaluation of Glycolipids Plakosides A, B and Their Analogs, K.C. Nicolaou, J. Li, G. Zenke, Helv. Chim. Acta 2000, 83, 1977–2006.

483. Model Studies Towards Diazonamide A: Synthesis of the Heterocyclic Core, K.C. Nicolaou, S.A. Snyder, K.B. Simonsen, K.E. Koumbis, Angew. Chem. Int. Ed. 2000, 39, 3473–3478.

484. Natural Product-like Combinatorial Libraries Based on Privileged Structures. 1.  General Principles and Solid-Phase Synthesis of Benzopyrans, K.C. Nicolaou, J.A. Pfefferkorn, A.J. Roecker, G.-Q. Cao, S. Barluenga, H.J. Mitchell, J. Am. Chem. Soc. 2000, 122, 9939–9953.

485. Natural Product-like Combinatorial Libraries Based on Privileged Structures. 2. Construction of a 10,000-Membered Benzopyran Library by Directed Split-and-Pool Chemistry Using NanoKans and Optical Encoding, K.C. Nicolaou, J.A. Pfefferkorn, H.J. Mitchell, A.J. Roecker, S. Barluenga, G.-Q. Cao, R.L. Affleck, J.E. Lillig, J. Am. Chem. Soc. 2000, 122, 9954–9967.

486. Natural Product-like Combinatorial Libraries Based on Privileged Structures. 3.  The "Libraries from Libraries" Principle for Diversity Enhancement of Benzopyran Libraries, K.C. Nicolaou, J.A. Pfefferkorn, S. Barluenga, H.J. Mitchell, A.J. Roecker, G.-Q. Cao, J. Am. Chem. Soc. 2000, 122, 9968–9976.

487. Novel Solution- and Solid-Phase Chemistry of a-Sulfonated Ketones Applicable to Combinatorial Chemistry, K.C. Nicolaou, P.S. Baran, Y.-L. Zhong, J. Am. Chem. Soc. 2000, 122, 10246–10248.

488. Target-Accelerated Combinatorial Synthesis and Discovery of Highly Potent Antibiotics Effective against Vancomycin-Resistant Bacteria, K.C. Nicolaou, R. Hughes, S.-Y. Cho, N. Winssinger, C. Smethurst, H. Labischinski, R. Endermann, Angew. Chem. Int. Ed. 2000, 39, 3823–3828.

489. New Roads to Molecular Complexity, K.C. Nicolaou, E.W. Yue, in The New Chemistry, Nina Hall, Ed., Cambridge University Press, Cambridge, UK, Ch. 8, 2000, pp. 168–198.

490. Combinatorial Synthesis of Novel and Potent Inhibitors of NADH: Ubiquinone Oxidoreductase, K.C. Nicolaou, J.A. Pfefferkorn, F. Schuler, A.J. Roecker, G.-Q. Cao, J.E. Casida, Chem. Biol. 2000, 7, 979–992.

491. Synthesis and Biological Evaluation of 12,13-Cyclopropyl and 12,13-Cyclobutyl Epothilones, K.C. Nicolaou, K. Namoto, J. Li, A. Ritzén, T. Ulven, M. Shoji, D. Zaharevitz, R. Gussio, D.L. Sackett, R.D. Ward, A. Hensler, T. Fojo, P. Giannakakou, ChemBioChem 2001, 2, 69–75.

492. Mechanistic Studies of Periodinane-Mediated Reactions of Anilides and Related Systems, K.C. Nicolaou, P.S. Baran, R. Kranich, Y.-L. Zhong, K. Sugita, N. Zou, Angew. Chem. Int. Ed. 2001, 40, 202–206.

493. New Synthetic Technology for the Construction of N-Containing Quinones and Derivatives Thereof. Total Synthesis of Epoxyquinomycin B, K.C. Nicolaou, K. Sugita, P.S. Baran, Y.-L. Zhong, Angew. Chem. Int. Ed. 2001, 40, 207–210.

494. High-Output Solid Phase Synthesis of Discrete Compounds Using Directed Split-and-Pool Strategy, R. Li, X.-Y. Xiao, K.C. Nicolaou in High-Throughput Synthesis, 1st Edition, I. Sucholeiki, Ed., Marcel Dekker, Inc., New York, Ch. 6-4, 2001, pp. 207–213.

495. Does CIP Nomenclature Adequately Handle Molecules with Multiple Stereoelements?  A Case Study of Vancomycin and Cognates, K.C. Nicolaou, C.N.C. Boddy, J.S. Siegel, Angew. Chem. Int. Ed. 2001, 40, 701–704.

496. Total Synthesis of Hybocarpone, K.C. Nicolaou, D. Gray, Angew. Chem. Int. Ed. 2001, 40, 761–763.

497. Synthesis of the FGHI Ring System of Azaspiracid, K.C. Nicolaou, P.M. Pihko, N. Diedrichs, N. Zou, F. Bernal, Angew Chem. Int. Ed. 2001, 40, 1262–1265.

498. Selective Oxidation at Carbon Adjacent to Aromatic Systems with IBX, K.C. Nicolaou, P.S. Baran, Y.-L. Zhong, J. Am. Chem. Soc. 2001, 123, 3183–3185.

499. Behind Enemy Lines, K.C. Nicolaou, C.N.C. Boddy, Sci. Am. 2001, 284, 46–53.

500. Adventures in Carbohydrate Chemistry: New Synthetic Technologies, Chemical Synthesis, Molecular Design and Chemical Biology, K.C. Nicolaou, H.J. Mitchell, Angew. Chem. Int. Ed. 2001, 40, 1576–1624.

501. A New Photolabile Linker for the Photoactivation of Carboxyl Groups, K.C. Nicolaou, B.S. Safina, N. Winssinger, Synlett 2001, 900–903.

502. Rapid Access to Complex Molecular Architectures via a-Azaquinones, K.C. Nicolaou, Y.-L. Zhong, P.S. Baran, K. Sugita, Angew Chem. Int. Ed. 2001, 40, 2145–2149.

503. Discovery of Novel Antibacterial Agents Active Against Methicillin-Resistant Staphylococcus aureus (MRSA) from Combinatorial Benzopyran Libraries, K.C. Nicolaou, A.J. Roecker, S.B. Barluenga, J.A. Pfefferkorn, G.-Q. Cao, ChemBioChem 2001, 2, 460–465.

504. An Expedient Synthesis to D-Callipeltose, A.J. Pihko, K.C. Nicolaou, A.M.P. Koskinen, Tetrahedron: Asymmetry 2001, 12, 937–942.

505. Total Synthesis of Colombiasin A, K.C. Nicolaou, G. Vassilikogiannakis, W. Mägerlein, R. Kranich, Angew Chem. Int. Ed. 2001, 40, 2482–2486.

506. Solid- and Solution-Phase Synthesis of Vancomycin and Vancomycin Analogues with Activity Against Vancomycin-Resistant Bacteria, K.C. Nicolaou, S.Y. Cho, R. Hughes, N. Winssinger, C. Smethurst, H. Labischinski, R. Endermann, Chem. Eur. J. 2001, 7, 3798–3823.

507. Synthesis and Biological Evaluation of Vancomycin Dimers with Potent Activity Against Vancomycin-Resistant Bacteria. Target-Accelerated Combinatorial Synthesis, K.C. Nicolaou, R. Hughes, S.Y. Cho, N. Winssinger, H. Labischinski, R. Endermann Chem. Eur. J. 2001, 7, 3824–3843.

508. Recent Developments in the Chemistry, Biology and Medicine of the Epothilones K.C. Nicolaou, A. Ritzén, K. Namoto, Chem. Commun. 2001, 1523–1535.

509. Chemical Synthesis and Biological Evaluation of cis- and trans-12,13-Cyclopropyl and 12,13-Cyclobutyl Epothilones and Related Pyridine Side Chain Analogues, K.C. Nicolaou, K. Namoto, A. Ritzén, T. Ulven, M. Shoji, J. Li, G. D’Amico, D. Liotta, C.T. French, M. Wartmann, K.-H. Altmann, P. Giannakakou, J. Am. Chem. Soc. 2001, 123, 9313–9323.

510. Antitumor Efficacy of 26-Fluoroepothilone B Against Human Prostate Cancer Xenografts, R.A. Newman, J. Yang, M.R.V. Finlay, F. Cabral, D. Vourloumis, C. Stevens, P. Troncoso, X. Wu, C.J. Logothetis, K.C. Nicolaou, N.M. Navone, Cancer Chemother. Pharmacol. 2001, 48, 319–326.

511. Total Synthesis of Hamigerans: Part 1. Development of Synthetic Technology for the Construction of Benzannulated Polycyclic Systems by the Intramolecular Trapping of Photogenerated Hydroxy-o-quinodimethanes and Synthesis of Key Building Blocks, K.C. Nicolaou, D. Gray, J. Tae, Angew Chem. Int. Ed. 2001, 40, 3675–3678.

512. Total Synthesis of Hamigerans: Part 2. Implementation of the Intramolecular Diels–Alder Trapping of Photochemically Generated Hydroxy-o-quinodimethanes; Strategy and Completion of the Synthesis, K.C. Nicolaou, D. Gray, J. Tae, Angew Chem. Int. Ed. 2001, 40, 3679–3683.

513. Total Synthesis of Apoptolidin–Part 1: Retrosynthetic Analysis and Construction of Building Blocks, K.C. Nicolaou, Y. Li, K.C. Fylaktakidou, H.J. Mitchell, H.-X. Wei, B. Weyershausen, Angew. Chem. Int. Ed. 2001, 40, 3849–3854.

514. Total Synthesis of Apoptolidin–Part 2: Coupling of Key Building Blocks and Completion of the Synthesis, K.C. Nicolaou, Y. Li, K.C. Fylaktakidou, H.J. Mitchell, K. Sugita, Angew. Chem. Int. Ed. 2001, 40, 3854–3857.

515. Combinatorial Synthesis through Disulfide Exchange:  Discovery of Potent Psammaplin A Type Antibacterial Agents Active Against Methicillin-Resistant Staphylococcus aureus (MRSA), K.C. Nicolaou, R. Hughes, J.A. Pfefferkorn, S. Barluenga, A.J. Roecker, Chem. Eur. J. 2001, 7, 4280–4295.

516. Optimization and Mechanistic Studies of Psammaplin A Type Antibacterial Agents Active Against Methicillin-Resistant Staphylococcus aureus (MRSA), K.C. Nicolaou, R. Hughes, J.A. Pfefferkorn, S. Barluenga, Chem. Eur. J. 2001, 7, 4296–4310.

517. Synthesis of the ABCD Ring System of Azaspiracid, K.C. Nicolaou, W. Qian, F. Bernal, N. Uesaka, P.M. Pihko, J. Hinrichs, Angew. Chem. Int. Ed. 2001, 40, 4068–4071.

518. cis-3,4-Dichlorocyclobutene as a Versatile Synthon in Organic Synthesis. Rapid Entry into Complex Polycyclic Systems with Remarkably Stereospecific Reactions, K.C. Nicolaou, J.A. Vega, G. Vassilikogiannakis, Angew. Chem. Int. Ed. 2001, 40, 4441–4445.

519. Epothilones and Sarcodictyins: From Combinatorial Libraries to Designed Analogs, N. Winssinger, K.C. Nicolaou, in New Prospects in Anticancer Agents for the 21st Century, 219th ACS National Meeting Symposium New Prospects, Special Issue, No. 900, 2001, pp. 148–170.

520. “Biomimetic” Cascade Reactions in Organic Synthesis: Construction of 4-Oxatricyclo[4.3.1.0]decan-2-one Systems and Total Synthesis of 1-O-Methylforbesione via Tandem Claisen Rearrangement/Diels–Alder Reactions, K.C. Nicolaou, J. Li, Angew. Chem. Int. Ed. 2001, 40, 4264–4268.

521. Total Synthesis of Colombiasin A and Determination of Its Absolute Configuration, K.C. Nicolaou, G. Vassilikogiannakis, W. Mägerlein, R. Kranich, Chem. Eur. J. 2001, 7, 5359–5371.

522. Solid Phase Synthesis of Complex Natural Products and Libraries Thereof, K.C. Nicolaou, J.A. Pfefferkorn, Biopolymers Peptide Science 2001, 60, 171–193.

523. Construction of the Complete Aromatic Core of Diazonamide A via a Novel Hetero Pinacol Macrocyclization Cascade Reaction, K.C. Nicolaou, X. Huang, N. Giuseppone, P. Bheema Rao, M. Bella, M.V. Reddy, S.A. Snyder, Angew. Chem. Int. Ed. 2001, 40, 4705–4709.

524. A Novel Regio- and Stereoselective Synthesis of Sulfamidates from 1,2-Diols Using Burgess and Related Reagents: A Facile Entry into b-Amino Alcohols, K.C. Nicolaou, X. Huang, S.A. Snyder, P. Bheema Rao, M. Bella, M.V. Reddy, Angew. Chem. Int. Ed. 2002, 41, 834–838.

525. Total Synthesis of the CP-Molecules (CP-263,114 and CP-225,917, Phomoidrides B and A). 1. Racemic and Asymmetric Synthesis of Bicyclo[4.3.1] Key Building Blocks, K.C. Nicolaou, J. Jung, W.H. Yoon, K.C. Fong, H.-S. Choi, Y. He, Y.-L. Zhong, P.S. Baran, J. Am. Chem. Soc. 2002, 124, 2183–2189.

526. Total Synthesis of the CP-Molecules (CP-263,114 and CP-225,917, Phomoidrides B and A). 2. Model Studies for the Construction of Key Structural Elements and First Generation Strategy, K.C. Nicolaou, P.S. Baran, Y.-L. Zhong, K.C. Fong, H.-S. Choi, J. Am. Chem. Soc. 2002, 124, 2190–2201.

527. Total Synthesis of the CP-Molecules (CP-263,114 and CP-225,917, Phomoidrides B and A). 3. Completion and Synthesis of Advanced Analogs, K.C. Nicolaou, Y.-L. Zhong, P.S. Baran, J. Jung, H.-S. Choi, W.H. Yoon, J. Am. Chem. Soc. 2002, 124, 2202–2211.

528. Iodine(V) Reagents in Organic Synthesis. Part 1. Synthesis of Polycyclic Heterocycles via DMP-Mediated Cascade Cyclization: Generality, Scope and Mechanism of the Reaction, K.C. Nicolaou, P.S. Baran, Y.-L. Zhong, K. Sugita, J. Am. Chem. Soc. 2002, 124, 2212–2220.

529. Iodine(V) Reagents in Organic Synthesis. Part 2. Access to Complex Molecular Architectures via DMP-Generated o-Imidoquinones, K.C. Nicolaou, K. Sugita, P.S. Baran, Y.-L. Zhong, J. Am. Chem. Soc. 2002, 124, 2221–2232.

530. Iodine(V) Reagents in Organic Synthesis. Part 3. New Routes to Heterocyclic Compounds via IBX-Mediated Cyclizations: Generality, Scope, and Mechanism, K.C. Nicolaou, P.S. Baran, Y.-L. Zhong, S. Barluenga, K.W. Hunt, R. Kranich, J.A. Vega, J. Am. Chem. Soc. 2002, 124, 2233–2244.

531. Iodine(V) Reagents in Organic Synthesis. Part 4. IBX as a Chemospecific Tool for SET-Based Oxidation Processes, K.C. Nicolaou, T. Montagnon, P.S. Baran, Y.-L. Zhong, J. Am. Chem. Soc. 2002, 124, 2245–2258.

532. Modulation of the Reactivity Profile of IBX by Ligand Complexation: Ambient Temperature Dehydrogenation of Aldehydes and Ketones to a,b-Unsaturated Carbonyl Compounds, K.C. Nicolaou, T. Montagnon, P.S. Baran, Angew. Chem. Int. Ed. 2002, 41, 993–996.

533. Oxidation of Silyl Enol Ethers by Using IBX and IBX·N-Oxide Complexes: A Mild and Selective Reaction for the Synthesis of Enones, K.C. Nicolaou, D.L.F. Gray, T. Montagnon, S.T. Harrison, Angew. Chem. Int. Ed. 2002, 41, 996–1000.

534. HIO3 and I2O5: Mild and Selective Alternative Reagents to IBX for the Dehydrogenation of Aldehydes and Ketones, K.C. Nicolaou, T. Montagnon, P.S. Baran, Angew. Chem. Int. Ed. 2002, 41, 1386–1389. [Corrigendum/Warning: Angew. Chem. Int. Ed. 2003, 42, 3981].

535. Novel Chemistry of a-Tosyloxy Ketones: Applications to the Solution- and Solid-Phase Synthesis of Privileged Heterocycle and Enediyne Libraries, K.C. Nicolaou, T. Montagnon, T. Ulven, P.S. Baran, Y.-L. Zhong, F. Sarabia, J. Am. Chem. Soc. 2002, 124, 5718–5728.

536. The Diels–Alder Reaction in Total Synthesis, K.C. Nicolaou, S.A. Snyder, T. Montagnon, G.E. Vassilikogiannakis, Angew. Chem. Int. Ed. 2002, 41, 1668–1698.

537. Stereocontrolled Synthesis of the Quinaldic Acid Macrocyclic System of Thiostrepton, K.C. Nicolaou, B.S. Safina, C. Funke, M. Zak, F.J. Zécri, Angew. Chem. Int. Ed. 2002, 41, 1937–1940.

538. A Biomimetically Inspired Synthesis of the Dehydropiperidine Domain of Thiostrepton, K.C. Nicolaou, M. Nevalainen, B.S. Safina, M. Zak, S. Bulat, Angew. Chem. Int. Ed. 2002, 41, 1941–1945.

539. Model Studies Towards Azadirachtin: Part 1. Construction of the Crowded C8-C14 Bond by Radical Chemistry, K.C. Nicolaou, M. Follmann, A.J. Roecker, K.W. Hunt, Angew. Chem. Int. Ed. 2002, 41, 2103–2106.

540. Model Studies Towards Azadirachtin: Part 2. Construction of the Crowded C8-C14 Bond by Transition Metal Chemistry, K.C. Nicolaou, A.J. Roecker, M. Follmann, R. Baati, Angew. Chem. Int. Ed. 2002, 41, 2107–2110.

541. The CP Molecule Labyrinth: A Paradigm of How Endeavors in Total Synthesis Lead to Discoveries and Inventions in Organic Synthesis, K.C. Nicolaou, P.S. Baran, Angew. Chem. Int. Ed. 2002, 41, 2678–2720.

542. Chemical Synthesis and Biological Evaluation of Novel Epothilone B and trans-12,13-Cyclopropyl Epothilone B Analogues, K.C. Nicolaou, A. Ritzén, K. Namoto, R.M. Buey, J. Fernando Díaz, J.M. Andreu, M. Wartmann, K.-H. Altmann, A. O’Brate, P. Giannakakou, Tetrahedron 2002, 58, 6413–6432.

543. Enhanced Microtubule-Dependent Trafficking and p53 Nuclear Accumulation by Suppresion of Microtubule Dynamics, P. Giannakakou, M. Nakano, K.C. Nicolaou, A. O’Brate, J. Yu, M.V. Blagosklonny, U.R. Greber, T. Fojo, Proc. Natl. Acad. Sci. USA 2002, 99, 10855–10860.

544. Total Synthesis of Coleophomones B and C, K.C. Nicolaou, G. Vassilikogiannakis, T. Montagnon, Angew. Chem. Int. Ed. 2002, 41, 3276–3281.

545. Atropselective Macrocyclization of Diaryl Ether Ring Systems: Application to the Synthesis of Vancomycin Model Systems, K.C. Nicolaou, C.N.C. Boddy, J. Am. Chem. Soc. 2002, 124, 10451–10455.

546. Total Synthesis of Diazonamide A, K.C. Nicolaou, M. Bella, D.Y.-K. Chen, X. Huang, T. Ling, S.A. Snyder, Angew. Chem. Int. Ed. 2002, 41, 3495–3499.

547. Stereocontrolled Total Synthesis of Apicularen A and Its Δ17,18 Z Isomer, K.C. Nicolaou, D.W. Kim, R. Baati, Angew. Chem. Int. Ed. 2002, 41, 3701–3704.

548. A New Method for the Synthesis of Non-Symmetrical Sulfamides Using Burgess-Type Reagents, K.C. Nicolaou, D.A. Longbottom, S.A. Snyder, A.Z. Nalbanadian X. Huang, Angew. Chem. Int. Ed. 2002, 41, 3866–3870.

549. Total Synthesis of Coleophomone D, K.C. Nicolaou, T. Montangon, G. Vassilikogiannakis, Chem. Commun. 2002, 2478–2479.

550. An Expedient Entry into the Fused Polycyclic Skeleton of Vannusal A, K.C. Nicolaou M.P. Jennings, P. Dagneau, Chem. Commun. 2002, 2480–2481.

551. Bromotyrosine-Derived Natural and Synthetic Products as Inhibitors of Mycothiol-S-Conjugate Amidase, L.L. Eckman, G.M. Nicholas, R.O. Hughes, J.A. Pfefferkorn, S. Barluenga, K.C. Nicolaou, C.A. Bewley, Bioorg. Med. Chem. Lett. 2002, 12, 2487–2490.

552. Chemistry, Biology and Medicine in the 21st Century, K.C. Nicolaou, A.E. Koumbis, in Science, Frontier Technology, and Orthodoxy, Proceedings to the Biomedical Ethic Symposium, Holy Church of Greece, Athens, 2002, pp. 177–193 (Review in Greek; Book).

553. Protracted Low-Dose Effects on Human Endothelial Cell Proliferation and Survival in Vitro Reveal a Selective Antiangiogenic Window for Various Chemotherapeutic Drugs, G. Bocci, K.C. Nicolaou, R.S. Kerbel, Cancer Res. 2002, 62, 6938–6943.

554. Novel Strategies for the Solid Phase Synthesis of Substituted Indolines and Indoles, K.C. Nicolaou, A.J. Roecker, R. Hughes, R. van Summeren, J.A. Pfefferkorn, N. Winssinger, Bioorg. Med. Chem. 2003, 11, 465–476.

555. Tandem Reactions, Cascade Sequences, and Biomimetic Strategies in Total Synthesis, K.C. Nicolaou, T. Montagnon, S.A. Snyder, Chem. Commun. 2003, 551–564.

556. Discovery and Optimization of Non-Steroidal FXR Agonists from Natural Product-Like Libraries, K.C. Nicolaou, R.M. Evans, A.J. Roecker, R. Hughes, M. Downes, J.A. Pfefferkorn, Org. Biomol. Chem. 2003, 1, 908–920.

557. The Second Total Synthesis of Diazonamide A, K.C. Nicolaou, P.B. Rao, J. Hao, M.V. Reddy, G. Rassias, X. Huang, D.Y.-K. Chen, S.A. Snyder, Angew. Chem. Int. Ed. 2003, 42, 1753–1758.

558. A Chemical, Genetic and Structural Analysis of the Nuclear Bile Acid Receptor FXR, M. Downes, M. Verdecia, A.J. Roecker, R. Hughes, J.B. Hogenesch, H.R. Kast-Woelbern, M.E. Bowman, J.-L. Ferrer, A.M. Anisfeld, P.A. Edwards, J.M. Rosenfeld, J.G.A. Alvarez, J.P. Noel, K.C. Nicolaou, R.M. Evans, Mol. Cell 2003, 11, 1079–1092.

559. Cascade Reactions in Total Synthesis. Recent Advances, K.C. Nicolaou, S.A. Snyder, L’Actualite Chimique 2003, 83–88.

560. Natural Products and Chemical Synthesis at the Forefront of the Fight Against Cancer, K.C. Nicolaou, T. Montagnon, G.E. Vassilikogiannakis, Bio 2003, April–June (5), 22–30. (Greek)

561. Synthetic Studies on Thiostrepton: Construction of Thiostrepton Analogues with the Thiazoline-Containing Macrocycle, K.C. Nicolaou, M. Nevalainen, M. Zak, S. Bulat, M. Bella, B.S. Safina, Angew. Chem. Int. Ed. 2003, 42, 3418–3424.

562. Design, Synthesis and Biological Properties of Highly Potent Epothilone B Analogs, K.C. Nicolaou, P.K. Sasmal, G. Rassias, M.V. Reddy, K.-H. Altmann, M. Wartmann, A. O’Brate, P. Giannakakou, Angew. Chem. Int. Ed. 2003, 42, 3515–3520.

563. Synthesis of Complex Carbohydrates: Everninomicin 13,384-1, K.C. Nicolaou, H.J. Mitchell, S.A. Snyder, in Carbohydrate-based Drug Discovery, Vol. 1, C.-H.Wong, Ed., Wiley-VCH, Weinheim, Ch. 8, 2003, pp. 215–252.

564. Studies Towards the Synthesis of Azadirachtin: Enantioselective Entry Into the Azadirachtin Framework Through Cascade Reactions, K.C. Nicolaou, A.J. Roecker, H. Monenschein, P. Guntupalli, M. Follmann, Angew. Chem. Int. Ed. 2003, 42, 3637–3642.

565. Total Synthesis of the Proposed Azaspiracid-1 Structure, Part 1: Construction of Enantiomerically Pure C1–C20, C21–C27 and C28–C40 Fragments, K.C. Nicolaou, Y. Li, N. Uesaka, T.V. Koftis, S. Vyskocil, T. Ling, M. Govindasamy, W. Qian, F. Bernal, D.Y.-K. Chen, Angew. Chem. Int. Ed. 2003, 42, 3643–3648.

566. Total Synthesis of the Proposed Azaspiracid-1 Structure, Part 2: Coupling of C1–C20, C21–C27 and C28–C40 Fragments and Completion of the Synthesis, K.C. Nicolaou, D.Y.-K. Chen, Y. Li, W. Qian, T. Ling, S. Vyskocil, T.V. Koftis, M. Govindasamy, N. Uesaka, Angew. Chem. Int. Ed. 2003, 42, 3649–3653.

567. Perspectives in Total Synthesis: A Personal Account, K.C. Nicolaou, Tetrahedron 2003, 59, 6683–6738.

568. The Olefin Metathesis Reaction in Complex Molecule Construction, K.C. Nicolaou, S.A. Snyder, in Handbook of Metathesis, Vol. 2, R.H. Grubbs, Ed., Wiley-VCH, Weinheim, Ch. 2.9, 2003, pp. 323–337.

569. New Reactions of IBX: Oxidation of Nitrogen- and Sulfur-Containing Substrates to Afford Useful Synthetic Intermediates, K.C. Nicolaou, C.J.N. Mathison, T. Montagnon, Angew. Chem. Int. Ed. 2003, 42, 4077–4082.

570. Total Synthesis of 1-O-Methyllateriflorone, K.C. Nicolaou, P.K. Sasmal, H. Xu, K. Namoto, A. Ritzén, Angew. Chem. Int. Ed. 2003, 42, 4225–4229.

571. Total Synthesis and Biological Evaluation of (–)-Apicularen A and Analogs Thereof, K.C. Nicolaou, D.W. Kim, R. Baati, A. O’Brate, P. Giannakakou, Chem. Eur. J. 2003, 9, 6177–6191.

572. Total Synthesis of Apoptolidin: Construction of Enantiomerically Pure Fragments, K.C. Nicolaou, K.C. Fylaktakidou, H. Monenschein, Y. Li, B. Weyershausen, H.J. Mitchell, H. Wei, P. Guntupalli, D. Hepworth, K. Sugita, J. Am. Chem. Soc. 2003, 125, 15433–15442.

573. Total Synthesis of Apoptolidin: Completion of the Synthesis and Analogue Synthesis and Evaluation, K.C. Nicolaou, Y. Li, K. Sugita, H. Monenschein, P. Guntupalli, H.J. Mitchell, K.C. Fylaktakidou, D. Vourloumis, P. Giannakakou, A. O’Brate, J. Am. Chem. Soc. 2003, 125, 15443–15454.

574. Total Synthesis of Hybocarpone and Analogues Thereof. A Facile Dimerization of Naphthazarins to Pentacyclic Systems, K.C. Nicolaou, D.L.F. Gray, J. Am. Chem. Soc. 2004, 126, 607–612.

575. Total Synthesis of Hamigerans and Analogues Thereof. Photochemical Generation and Diels-Alder Trapping of Hydroxy-o-quinodimethanes, K.C. Nicolaou, D.L.F. Gray, J. Tae, J. Am. Chem. Soc. 2004, 126, 613–627.

576. Interaction of Epothilone Analogs with the Paclitaxel Binding Site: Relationship Between Binding Affinity, Microtubule Stabilization, and Cytotoxicity, R.M. Buey, J.F. Díaz, J.M. Andreu, A. O’Brate, P. Giannakakou, K.C. Nicolaou, P.K. Sasmal, A. Ritzén, K. Namoto, Chem. Biol. 2004, 11, 225–236.

577. o-Iodoxybenzoic Acid (IBX) as a Viable Reagent in the Manipulation of Nitrogen- and Sulfur-Containing Substrates: Scope, Generality and Mechanism of IBX-Mediated Amine Oxidations and Dithiane Deprotections, K.C. Nicolaou, C.J.N. Mathison, T. Montagnon, J. Am. Chem. Soc. 2004, 126, 5192–5201.

578. Biomimetically Inspired Total Synthesis and Structure Activity Relationships of 1-O-Methyllateriflorone. 6π Electrocyclizations in Organic Synthesis, K.C. Nicolaou, P.K. Sasmal, H. Xu, J. Am. Chem. Soc. 2004, 126, 5493–5501.

579. A New Method for the Stereoselective Synthesis of α- and β-Glycosylamines Using the Burgess Reagent, K.C. Nicolaou, S.A. Snyder, A.Z. Nalbandian, D.A. Longbottom, J. Am. Chem. Soc. 2004, 126, 6234–6235.

580. Structural Revision and Total Synthesis of Azaspiracid-1. Part 1: Intelligence Gathering and Tentative Proposal, K.C. Nicolaou, S. Vyskocil, T.V. Koftis, Y.M.A. Yamada, T. Ling, D.Y.-K. Chen, W. Tang, G. Petrovic, M.O. Frederick, Y. Li, M. Satake, Angew. Chem. Int. Ed. 2004, 43, 4312–4318.

581. Structural Revision and Total Synthesis of Azaspiracid-1. Part 2: Definition of the ABCD Domain and Total Synthesis, K.C. Nicolaou, T.V. Koftis, S. Vyskocil, G. Petrovic, T. Ling, Y.M.A. Yamada, W. Tang, M.O. Frederick, Angew. Chem. Int. Ed. 2004, 43, 4318–4324.

582. The Essence of Total Synthesis, K.C. Nicolaou, S.A. Snyder, Proc. Natl. Acad. Sci. USA 2004, 101, 11929–11936.

583. Studies Toward Diazonamide A: Initial Synthetic Forays Directed Toward the Originally Proposed Structure, K.C. Nicolaou, S.A. Snyder, X. Huang, K.B. Simonsen, A.E. Koumbis, A. Bigot, J. Am. Chem. Soc. 2004, 126, 10162–10173.

584. Studies Toward Diazonamide A: Development of a Hetero Pinacol Macrocyclization Cascade for the Construction of the Bis-Macrocyclic Framework of the Originally Proposed Structure, K.C. Nicolaou, S.A. Snyder, N. Giuseppone, X. Huang, M. Bella, M.V. Reddy, P. Bheema Rao, A.E. Koumbis, P. Giannakakou, A. O’Brate, J. Am. Chem. Soc. 2004, 126, 10174–10182.

585. Chemistry and Biology of Diazonamide A: First Total Synthesis and Confirmation of the True Structure, K.C. Nicolaou, D.Y.-K. Chen, X. Huang, T. Ling, M. Bella, S.A. Snyder, J. Am. Chem. Soc. 2004, 126, 12888–12896.

586. Chemistry and Biology of Diazonamide A: Second Total Synthesis of Diazonamide A and Biological Investigations, K.C. Nicolaou, J. Hao, M.V. Reddy, P. Bheema Rao, G. Rassias, S.A. Snyder, X. Huang, D.Y.-K. Chen, W.E. Brenzovich, N. Giuseppone, P. Giannakakou, A. O’Brate, J. Am. Chem. Soc. 2004, 126, 12897–12906.

587. Total Synthesis of Thiostrepton, Part 1: Construction of the Dehydropiperidine Thiazoline-Containing Macrocycle, K.C. Nicolaou, B.S. Safina, M. Zak, A.A. Estrada, S.H. Lee, Angew. Chem. Int. Ed. 2004, 43, 5087–5092.

588. Total Synthesis of Thiostrepton, Part 2: Construction of the Quinaldic Acid-Containing Macrocycle and Completion of the Synthesis, K.C. Nicolaou, M. Zak, B.S. Safina, S.H. Lee, A.A. Estrada, Angew. Chem. Int. Ed. 2004, 43, 5092–5097.

589. New Uses for the Burgess Reagent in Chemical Synthesis: Methods for the Facile and Stereoselective Formation of Sulfamidates, Glycosylamines, and Sulfamides, K.C. Nicolaou, S.A. Snyder, D.A. Longbottom, A.Z. Nalbandian, X. Huang, Chem. Eur. J. 2004, 10, 5581–5606.

590. Biomimetic Total Synthesis of Gambogin and Rate Acceleration of Pericyclic Reactions in Aqueous Media, K.C. Nicolaou, H. Xu, M. Wartmann, Angew. Chem. Int. Ed. 2005, 44, 756–761.

591. Chasing Molecules That Were Never There: Misassigned Natural Products and the Role of Chemical Synthesis in Modern Structure Elucidation, K.C. Nicolaou, S.A. Snyder, Angew. Chem. Int. Ed. 2005, 44, 1012–1044. [Corrigendum: Angew. Chem. Int. Ed. 2005, 44, 2050].

592. A Mild and Selective Method for the Hydrolysis of Esters Employing Trimethyltin Hydroxide, K.C. Nicolaou, A.A. Estrada, M. Zak, S.H. Lee, B.S. Safina, Angew. Chem. Int. Ed. 2005, 44, 1378–1382.

593. Identification of a Novel Small Molecule Inhibitor of the Hypoxia-Inducible Factor 1 Pathway, C. Tan, R.G. de Noronha, A.J. Roecker, B. Pyrzynska, F. Khwaja, Z. Zhang, H. Zhang, Q. Teng, A.C. Nicholson, P. Giannakakou, W. Zhou, J.J. Olson, M.M. Pereira, K.C. Nicolaou, E.G. Van Meir, Cancer Res. 2005, 65, 605–612.

594. Studies Toward the Synthesis of Azadirachtin, Part 1:  Total Synthesis of a Fully Functionalized ABC Ring Framework and Coupling with a Norbornene Domain, K.C. Nicolaou, P.K. Sasmal, A.J. Roecker, X.-W. Sun, S. Mandal, A. Converso, Angew. Chem. Int. Ed. 2005, 44, 3443–3447.

595. Studies Toward the Synthesis of Azadirachtin, Part 2: Construction of Fully Functionalized ABCD Ring Frameworks and Unusual Intramolecular Reactions Induced by Close-Proximity Effects, K.C. Nicolaou, P.K. Sasmal, T.V. Koftis, A. Converso, E. Loizidou, F. Kaiser, A.J. Roecker, K. Dellios, X.-W. Sun, G. Petrovic, Angew. Chem. Int. Ed. 2005, 44, 3447–3452.

596. Construction of Substituted N-Hydroxyindoles:  Synthesis of a Nocathiacin I Model System, K.C. Nicolaou, S.H. Lee, A.A. Estrada, M. Zak, Angew. Chem. Int. Ed. 2005, 44, 3736–3740.

597. A Catalytic Asymmetric Three-Component 1,4-Addition/Aldol Reaction: Enantioselective Synthesis of the Spirocyclic System of Vannusal A, K.C. Nicolaou, W. Tang, P. Dagneau, R. Faraoni, Angew. Chem. Int. Ed. 2005, 44, 3874–3879.

598. Construction of Highly Functionalized Medium-Sized Rings: Synthesis of Hyperforin and Perforatumone Model Systems, K.C. Nicolaou, G.E.A. Carenzi, V. Jeso, Angew. Chem. Int. Ed. 2005, 44, 3895–3899.

599. The Total Synthesis of Coleophomones B, C, and D, K.C. Nicolaou, T. Montagnon, G. Vassilikogiannakis, C.J.N. Mathison, J. Am. Chem. Soc. 2005, 127, 8872–8888.

600. Palladium-Catalyzed Cross-Coupling Reactions in Total Synthesis, K.C. Nicolaou, P.G. Bulger, D. Sarlah, Angew. Chem. Int. Ed. 2005, 44, 4442–4489.

601. Metathesis Reactions in Total Synthesis, K.C. Nicolaou, P.G. Bulger, D. Sarlah, Angew. Chem. Int. Ed. 2005, 44, 4490–4527.

602. Total Synthesis of Halipeptins A and D and Analogues, K.C. Nicolaou, D.W. Kim, D. Schlawe, D.E. Lizos, R.G. de Noronha, D.A. Longbottom, Angew. Chem. Int. Ed. 2005, 44, 4925–4929.

603. Total Synthesis of Halipeptins: Isolation of Halipeptin D and Synthesis of Oxazoline Halipeptin Analogues, K.C. Nicolaou, D. Schlawe, D.W. Kim, D.A. Longbottom, R.G. de Noronha, D.E. Lizos, R R. Manam, D.J. Faulkner, Chem. Eur. J. 2005, 11, 6197–6211.

604. Total Synthesis of Thiostrepton. Retrosynthetic Analysis and Construction of Key Building Blocks, K.C. Nicolaou, B.S. Safina, M. Zak, S.H. Lee, M. Nevalainen, M. Bella, A.A. Estrada, C. Funke, F.J. Zécri, S. Bulat, J. Am. Chem. Soc. 2005, 127, 11159–11175.

605. Total Synthesis of Thiostrepton. Assembly of Key Building Blocks and Completion of the Synthesis, K.C. Nicolaou, M. Zak, B.S. Safina, A.A. Estrada, S.H. Lee, M. Nevalainen, J. Am. Chem. Soc. 2005, 127, 11176–11183.

606. Joys of Molecules. 1. Campaigns in Total Synthesis, K.C. Nicolaou, J. Org. Chem. 2005, 70, 7007–7027.

607. Joys of Molecules. 2. Endeavors in Chemical Biology and Medicinal Chemistry, K.C. Nicolaou, J. Med. Chem. 2005, 48, 5613–5638.

608. The Cytoskyrin Cascade: A Facile Entry into Cytoskyrin A, Deoxyrubroskyrin, Rugulin, Skyrin, and Flavoskyrin Model Systems,K.C. Nicolaou, C.D. Papageorgiou, J.L. Piper, R.K. Chadha, Angew. Chem. Int. Ed. 2005, 44, 5846–5851.

609. Synthesis of Imides, N-Acyl Vinylogous Carbamates and Ureas, and Nitriles by Oxidation of Amides and Amines with Dess–Martin Periodinane, K.C. Nicolaou, C.J.N. Mathison, Angew. Chem. Int. Ed. 2005, 44, 5992–5997.

610. Discovery of a Biologically Active Thiostrepton Fragment, K.C. Nicolaou, M. Zak, S. Rahimipour, A.A. Estrada, S.H. Lee, A. O’Brate, P. Giannakakou, M.R. Ghadiri, J. Am. Chem. Soc. 2005, 127, 15042–15044.

611. Total Synthesis of (+)-Rugulosin and (+)-2,2′-epi-Cytoskyrin A through Cascade Reactions, K.C. Nicolaou, Y.H. Lim, C.D. Papageorgiou, J.L. Piper, Angew. Chem. Int. Ed. 2005, 44, 7917–7921.

612. Molecular Design and Chemical Synthesis of a Highly Potent Epothilone, K.C. Nicolaou, B.A. Pratt, S. Arseniyadis, M. Wartmann, A. O’Brate, P. Giannakakou, ChemMedChem 2006, 1, 41–44.

613. Total Synthesis and Structural Elucidation of Azaspiracid-1. Construction of Key Building Blocks for Originally Proposed Structure, K.C. Nicolaou, P.M. Pihko, F. Bernal, M.O. Frederick, W. Qian, N. Uesaka, N. Diedrichs, J. Hinrichs, T.V. Koftis, E. Loizidou, G. Petrovic, M. Rodriquez, D. Sarlah, N. Zou, J. Am. Chem. Soc. 2006, 128, 2244–2257.

614. Total Synthesis and Structural Elucidation of Azaspiracid-1. Synthesis-based Analysis of Originally Proposed Structures and Indication of Their Non-Identity to the Natural Product, K.C. Nicolaou, D.Y.-K. Chen, Y. Li, N. Uesaka, G. Petrovic, T.V. Koftis, F. Bernal, M.O. Frederick, M. Govindasamy, T. Ling, P.M. Pihko, W. Tang, S. Vyskocil, J. Am. Chem. Soc. 2006, 128, 2258–2267.

615. Total Synthesis and Structural Elucidation of Azaspiracid-1. Final Assignment and Total Synthesis of the Correct Structure of Azaspiracid-1, K.C. Nicolaou, T.V. Koftis, S. Vyskocil, G. Petrovic, W. Tang, M.O. Frederick, D.Y.-K. Chen, Y. Li, T. Ling, Y.M.A. Yamada, J. Am. Chem. Soc. 2006, 128, 2859–2872.

616. Total Synthesis of Floresolide B and Δ6,7-Z-Floresolide B, K.C. Nicolaou, H. Xu, Chem. Commun. 2006, 600–602.

617. Stereocontrolled Synthesis of Model Core Systems of Lomaiviticins A and B, K.C. Nicolaou, R.M. Denton, A. Lenzen, A. Li, D.J. Edmonds, R.R. Milburn, S.T. Harrison, Angew. Chem. Int. Ed. 2006, 45, 2076–2081.

618. Total Synthesis and Biological Evaluation of Halipeptins A and D and Analogues, K.C. Nicolaou, D.E. Lizos, D.W. Kim, D. Schlawe, R.G. de Noronha, D.A. Longbottom, M. Rodriquez, M. Bucci, G. Cirino, J. Am. Chem. Soc. 2006, 128, 4460–4470.

619. Origins of Selectivity in Pericyclic Reaction Cascades for the Synthesis of Gambogin and Lateriflorone, A.E. Hayden, K.C. Nicolaou, K.N Houk, Org. Lett. 2006, 8, 2989–2992.

620. Total Synthesis and Confirmation of the Revised Structures of Azaspiracid-2 and Azaspiracid-3, K.C. Nicolaou, M.O. Frederick, G. Petrovic, K.P. Cole, E.Z. Loizidou, Angew. Chem. Int. Ed. 2006, 45, 2609–2615.

621. Total Synthesis of Abyssomicin C and atrop-Abyssomicin C, K.C. Nicolaou, S.T. Harrison, Angew. Chem. Int. Ed. 2006, 45, 3256–3260.

622. Second Generation Total Synthesis of Azaspiracids-1, -2 and -3, K.C. Nicolaou, M.O. Frederick, E.Z. Loizidou, G. Petrovic, K.P. Cole, T.V. Koftis, Y.M.A. Yamada, Chem. Asian J. 2006, 12, 245–263.

623. Synthesis of Highly Substituted N-Hydroxyindoles through 1,5-Addition of Carbon Nucleophiles to In Situ Generated Unsaturated Nitrones, K.C. Nicolaou, A.A. Estrada, S.H. Lee, G.C. Freestone, Angew. Chem. Int. Ed. 2006, 45, 5364–5368.

624. Structure Toxicity Relationships of Synthetic Azaspiracid-1 and Analogs in Mice, E. Ito, M.O. Frederick, T.V. Koftis, W. Tang, G. Petrovic, T. Ling, K.C. Nicolaou, Harmful Algae 2006, 5 (October), 586–591.

625. Synthesis of iso-Epoxy-Amphidinolide N and des-Epoxy-Caribenolide I Structures. Initial Forays, K.C. Nicolaou, W.E. Brenzovich, P.G. Bulger, T.M. Francis, Org. Biomol. Chem. 2006, 4, 2119–2157.

626. Synthesis of iso-Epoxy-Amphidinolide N and des-Epoxy-Caribenolide I Structures. Revised Strategy and Final Stages, K.C. Nicolaou, P.G. Bulger, W.E. Brenzovich, Org. Biomol. Chem. 2006, 4, 2158–2183.

627. Azaspiracids Modulate Intracellular pH Levels in Human Lymphocytes, A. Alfonso, M.R. Vieytes, K. Ofuji, M. Satake, K.C. Nicolaou, M.O. Frederick, L.M. Botana, Biochem. Biophys. Res. Commun. 2006, 346, 1091–1099.

628. Total Synthesis of Marinomycins A–C, K.C. Nicolaou, A.L. Nold, R.R. Milburn, C.S. Schindler, Angew. Chem. Int. Ed. 2006, 45, 6527–6532.

629. Total Synthesis of Platensimycin, K.C. Nicolaou, A. Li, D.J. Edmonds, Angew. Chem. Int. Ed. 2006, 45, 7086–7090.

630. Cascade Reactions in Total Synthesis, K.C. Nicolaou, D.J. Edmonds, P.G. Bulger, Angew. Chem. Int. Ed. 2006, 45, 7134–7186.

631. Total Synthesis of Antibiotics GE2270A and GE2270T, K.C. Nicolaou, B. Zou, D.H. Dethe, D.B. Li, D.Y.-K. Chen, Angew. Chem. Int. Ed. 2006, 45, 7786–7792.

632. Asymmetric Reactions in Total Synthesis, K.C. Nicolaou, P.G. Bulger, in Asymmetric Synthesis – The Essentials, M. Christmann, S. Bräse,  Eds., Wiley-VCH, Weinheim, Part IV, Ch. 42, 2006, pp. 225–240.

633. Synergistic Effects of Peloruside A and Laulimalide with Taxoid Site Drugs, but Not with Each Other, on Tubulin Assembly, E. Hamel, B.W. Day, J.H. Miller, M.K. Jung, P.T. Northcote, A.K. Ghosh, D.P. Curran, M. Cushman, K.C. Nicolaou, I. Paterson, E.J. Sorensen, Mol. Pharm. 2006, 70, 1555–1564.

634. Cell Growth Inhibition and Actin Cytoskeleton Disorganization Induced by Azaspiracid-1  Structure–Activity Studies, N. Vilariño, K.C. Nicolaou, M.O. Frederick, E. Cagide, I.M. Ares, M.C. Louzao, M.R. Vieytes, L.M. Botana, Chem. Res. Toxicol. 2006, 19, 1459–1466.

635. Total Synthesis of Abyssomicin C, Atrop-abyssomicin C, and Abyssomicin D: Implications for Natural Origins of Atrop-abyssomicin C, K.C. Nicolaou, S.T. Harrison, J. Am. Chem. Soc. 2007, 129, 429–440.

636. Total Synthesis of Marinomycins A–C and of Their Monomeric Counterparts monomarinomycin A and iso-monomarinomycin A, K.C. Nicolaou, A.L. Nold, R.R. Milburn, C.S. Schindler, K.P. Cole, J. Yamaguchi, J. Am. Chem. Soc. 2007, 129, 1760–1768.

637. The Chemistry and Biology of Epothilones – The Wheel Keeps Turning, K.-H. Altmann, B. Pfeiffer, S. Arseniyadis, B.A. Pratt, K.C. Nicolaou, ChemMedChem 2007, 2, 396–423.

638. Effects of Azaspiracid-1, a Potent Cytotoxic Agent, on Primary Neuronal Cultures.  A Structure-Activity Relationship Study, C. Vale, K.C. Nicolaou, M.O. Frederick, B. Gomez-Limia, A. Alfonso, M.R. Vieytes, L.M. Botana, J. Med. Chem. 2007, 50, 356–363.

639. Total Syntheses of 2,2'-epi-Cytoskyrin A, Rugulosin and the Alleged Structure of Rugulin, K.C. Nicolaou, Y.H. Lim, J.L. Piper, C.D. Papageorgiou, J. Am. Chem. Soc. 2007, 129, 4001–4013.

640. Asymmetric Total Syntheses of Platensimycin, K.C. Nicolaou, D.J. Edmonds, A. Li, G.S. Tria, Angew. Chem. Int. Ed. 2007, 46, 3942–3945.

641. Formal Synthesis of (±)-Platensimycin, K.C. Nicolaou, Y. Tang, J. Wang, Chem. Commun. 2007, 1922–1923.

642. Structural Assignment and Total Synthesis of Azaspiracid-1, M.O. Frederick, K.P. Cole, G. Petrovic, E. Loizidou, K.C. Nicolaou, in Phycotoxins: Chemistry and Biochemistry Ed., L.M. Botana, Blackwell Publishing, Ames, Ch. 16, 2007, pp. 297–309.

643. Total Synthesis and Stereochemistry of Uncialamycin, K.C. Nicolaou, H. Zhang, J.S. Chen, J.J. Crawford, L. Pasunoori, Angew. Chem. Int. Ed. 2007, 46, 4704–4707.

644. Total Synthesis and Revised Structure of Biyouyanagin A, K.C. Nicolaou, D. Shaw, D. Sarlah, Angew. Chem. Int. Ed. 2007, 46, 4708–4711.

645. Adamantaplatensimycin: A Bioactive Analogue of Platensimycin, K.C. Nicolaou, T. Lister, R.M. Denton, A. Montero, D.J. Edmonds, Angew. Chem. Int. Ed. 2007, 46, 4712–4714.

646. Construction of the “Left domain” of Haplophytine, K.C. Nicolaou, U. Majumder, S. Philippe Roche, D. Y.-K. Chen, Angew. Chem. Int. Ed. 2007, 46, 4715–4718.

647. New Synthetic Technology for the Construction of N-Hydroxyindoles and Synthesis of Nocathiacin I Model Systems, K.C. Nicolaou, A.A. Estrada, G.C. Freestone, S.H. Lee, X.M. Alvarez-Mico, Tetrahedron 2007, 63, 6088–6114.

648. On the Structure of Maitotoxin, K.C. Nicolaou, M.O. Frederick, Angew. Chem. Int. Ed. 2007, 46, 5278–5282.

649. Irreversible Cytoskeletal Disarrangement is Independent of Caspase Activation During In Vitro Azaspiracid Toxicity in Human Neuroblastoma Cells, N. Vilariño, K.C. Nicolaou, M.O. Frederick, M.R. Vieytes, L.M. Botana, Biochem. Pharm. 2007, 74, 327–335.

650. Total Synthesis of the Originally Proposed and Revised Structures of Palmerolide A, K.C. Nicolaou, R. Guduru, Y.-P. Sun, B. Banerji, D.Y.-K. Chen, Angew. Chem. Int. Ed. 2007, 46, 5896–5900.

651. The c-Jun-N-Terminal Kinase is Involved in the Neurotoxic Effect of Azaspiracid-1, C. Vale, B. Gómez-Limia, K.C. Nicolaou, M.O. Frederick, M.R. Vieytes, L. M. Botana, Cell. Physiol. Biochem. 2007, 20, 957–966.

652. Cascade Reactions Involving Formal [2+2] Thermal Cycloadditions:  Total Synthesis of Artochamins F, H, I, and J, K.C. Nicolaou, T. Lister, R.M. Denton, C.F. Gelin, Angew. Chem. Int. Ed. 2007, 46, 7501–7505.

653. Total Synthesis of Kinamycins C, F, and J, K.C. Nicolaou, H. Li, A.L. Nold, D. Pappo, A. Lenzen, J. Am. Chem. Soc. 2007, 129, 10356–10357.

654. Metathesis Reactions in the Synthesis of Complex Molecules, K.C. Nicolaou, A. Ortiz, R.M. Denton, Chemistry Today 2007, 25, 70-76.

655. Total Synthesis and Antibacterial Properties of Carbaplatensimycin, K.C. Nicolaou, Y. Tang, J. Wang, A.F. Stepan, A. Li, A. Montero, J. Am. Chem. Soc. 2007, 129, 14850–14851.

656. Chemical Synthesis of the GHIJK Ring System and Further Experimental Support for the Originally Assigned Structure of Maitotoxin, K.C. Nicolaou, K.P. Cole, M.O. Frederick, R.J. Aversa, R.M. Denton, Angew. Chem. Int. Ed. 2007, 46, 8875–8879.

657. Asymmetric Synthesis and Biological Properties of Uncialamycin and 26-epi-Uncialamycin, K.C. Nicolaou, J.S. Chen, H. Zhang, A. Montero, Angew. Chem. Int. Ed. 2008, 47, 185-189.

658. A Chiral Pool Based Synthesis of Platensimycin, K.C. Nicolaou, D. Pappo, K.Y. Tsang, R. Gibe, D.Y.-K. Chen, Angew. Chem. Int. Ed. 2008, 47, 944-946.

659. Total Synthesis of Thiopeptide Antibiotics GE2270A, GE2270T, and GE2270C, K.C. Nicolaou, D.H. Dethe, G.Y.C. Leung, B. Zou, D.Y.-K. Chen, Chem. Asian J. 2008, 3, 413-429.

660. Synthesis of the Sporolide Ring Framework through a Cascade Sequence Involving an Intramolecular [4+2] Cycloaddition Reaction of an o-Quinone, K.C. Nicolaou, J. Wang, Y. Tang, Angew. Chem. Int. Ed. 2008, 47, 1432-1435.

661. Total Synthesis of Platencin, K.C. Nicolaou, G.S. Tria, D.J. Edmonds, Angew. Chem. Int. Ed. 2008, 47, 1780-1783.

662. Total Synthesis of the Originally Proposed and Revised Structures of Palmerolide A and Isomers Thereof, K.C. Nicolaou, Y.-P. Sun, R. Guduru, B. Banerji, D.Y.-K. Chen, J. Am. Chem. Soc. 2008 130, 3633-3644.

663. Total Synthesis of Complex Heterocyclic Natural Products, K.C. Nicolaou, J.S. Chen, Symposium in Print, 21st International Congress of Heterocyclic Chemistry, Pure Appl. Chem. 2008, 80, 727–742.

664. Total Synthesis of Artochamins F, H, I and J through Cascade Reactions, K.C. Nicolaou, T. Lister, R.M. Denton, C.F. Gelin, Tetrahedron 2008, 64, 4736–4757.

665. Chemical Synthesis of the GHIJKLMNO Ring System of Maitotoxin, K.C. Nicolaou, M.O. Frederick, A.C.B. Burtoloso, R.M. Denton, F. Rivas, K.P. Cole, R.J. Aversa, R. Gibe, T. Umezawa, T. Suzuki, J. Am. Chem. Soc. 2008, 130, 7466–7476.

666. Synthesis of Biologically Active Taxoids, K.C. Nicolaou, R.K. Guy in Chemistry and Molecular Aspects of Drug Design and Action, E. A. Rekka, P. N. Kourounakis, Eds., CRC Press, Boca Raton, Ch. 7, 2008, pp. 101–109.

667. An Expedient Strategy for the Synthesis of Tryptamines and Other Heterocycles, K.C. Nicolaou, A. Krasovskiy, V.É. Trépanier, D.Y.-K. Chen, Angew. Chem. Int. Ed. 2008, 47, 4217–4280.

668. Total Syntheses of Amythiamicins A, B and C, K.C. Nicolaou, D.H. Dethe, D.Y.-K. Chen, Chem. Commun. 2008, 2632–2634.

669. Chemical Synthesis and Biological Evaluation of Palmerolide A Analogues, K.C. Nicolaou, G.Y.C. Leung, D.H. Dethe, R. Guduru, Y.-P. Sun, C.S. Lim, D.Y.-K. Chen, J. Am. Chem. Soc. 2008, 130, 10019–10023.

670. Total Syntheses and Structural Revisions of α- and β-Diversonolic Esters and Total Syntheses of Diversonol and Blennolide C, K.C. Nicolaou, A. Li, Angew. Chem. Int. Ed. 2008, 47, 6579–6582.

671. Total Synthesis, Revised Structure, and Biological Evaluation of Biyouyanagin A and Analogues Thereof, K.C. Nicolaou, T.R. Wu, D. Sarlah, D. Shaw, E. Rowcliffe, D.R. Burton, J. Am. Chem. Soc. 2008, 130, 11114–11121.

672. An Expedient Asymmetric Synthesis of Platencin, K.C. Nicolaou, Q.-Y. Toh, D.Y.-K. Chen, J. Am. Chem. Soc. 2008, 130, 11292–11293. [Corrrection: J. Am. Chem. Soc. 2008, 130, 14016].

673. Cytotoxic Effect of Azaspiracid-2 and Azaspiracid-2-Methyl Ester in Cultured Neurons: Involvement of the c-Jun N-Terminal Kinase, C. Vale, C. Wandscheer, K.C. Nicolaou, M.O. Frederick, C. Alfonso, A. Alfonso, M.R. Vieytes, L.M. Botana, J. Neurosci. Res. 2008, 86, 2952–2962.

674. The Continuing Saga of the Marine Polyether Biotoxins, K.C. Nicolaou, M.O. Frederick, R.J. Aversa, Angew. Chem. Int. Ed. 2008, 47, 7182–7225.

675. Total Synthesis of (+)-Cortistatin, K.C. Nicolaou, Y.-P. Sun, X.-S. Peng, D. Polet, D.Y.-K. Chen, Angew. Chem. Int. Ed. 2008, 47, 7310–7313.

676. Azaspiracid Substituent at C1 Is Relevant to In Vitro Toxicity, N. Vilariño, K.C. Nicolaou, M.O. Frederick, E. Cagide, C. Alfonso, E. Alonso, M.R. Vieytes, L.M. Botana, Chem. Res. Toxicol. 2008, 21, 1823–1831.

677. Design, Synthesis and Biological Evaluation of Platensimycin Analogues with Varying Degrees of Molecular Complexity, K.C. Nicolaou, A.F. Stepan, T. Lister, A. Montero, G.S. Tria, C.I. Turner, Y. Tang, J. Wang, R.M. Denton, D.J. Edmonds, J. Am. Chem. Soc. 2008, 130, 13110–13119.

678. Total Synthesis of the Originally Assigned Structure of Vannusal B, K.C. Nicolaou, H. Zhang, A. Ortiz, P. Dagneau, Angew. Chem. Int. Ed. 2008, 47, 8605–8610.

679. A Concise Asymmetric Total Synthesis of Aspidophytine, K.C. Nicolaou, S.M. Dalby, U. Majumder, J. Am. Chem. Soc.2008, 130, 14942–14943.

680. Discoveries from the Abyss: The Abyssomicins and Their Total Synthesis, K.C. Nicolaou, S.T. Harrison, J.S. Chen, Synthesis 2009, 33–42.

681. Recent Advances in the Total Synthesis and Biology of Naturally Occurring Antibiotics, K.C. Nicolaou, J.S. Chen, D.J. Edmonds, A.A. Estrada, Angew. Chem. Int. Ed. 2009, 48, 660–719.

682. Inspirations, Discoveries, and Future Perspectives in Total Synthesis, K.C. Nicolaou, J. Org. Chem. 2009, 74, 951–972.

683. Total Synthesis of Tovophyllin B, J. Valer, K.C. Nicolaou, Tetrahedron Lett. 2009, 50, 1161–1163.

684. Enantioselective Intramolecular Friedel–Crafts Type a-Arylation of Aldehydes, K.C. Nicolaou, R. Reingruber, D. Sarlah, S. Bräse, J. Am. Chem. Soc. 2009, 131, 2086–2087.[Correction: J. Am. Chem. Soc. 2009, 131, 6640].

685. New Synthetic Technologies for the Construction of Heterocycles and Tryptamines, K.C. Nicolaou, A. Krasovskiy, U. Majumder, V.É. Trépanier, D.Y.-K. Chen, J. Am. Chem. Soc. 2009, 131, 3690–3699.

686. From Nature to the Laboratory and Into the Clinic, K.C. Nicolaou, J.S. Chen, S.M. Dalby, Bioorg. Med. Chem. (Symposium-in-Print) 2009, 17, 2290–2303.

687. Total Synthesis of Hopeahainol A and Hopeanol, K.C. Nicolaou, R.T. Wu, Q. Kang, D.Y.-K. Chen, Angew. Chem. Int. Ed. 2009, 48, 3440–3443.

688. Total Synthesis and Absolute Configuration of the Bisanthraquinone Antibiotic BE-43472B, K.C. Nicolaou, Y.H. Lim, J. Becker, Angew. Chem. Int. Ed. 2009, 48, 3444–3448.

689. Total Synthesis of Sporolide B, K.C. Nicolaou, Y. Tang, J. Wang, Angew. Chem. Int. Ed. 2009, 48, 3449–3453.

690. Monoclonal Antibodies with Orthogonaol Azaspiracid Epitopes, M.O. Frederick, S.D. Marin, K.D. Janda, K.C. Nicolaou, T.J. Dickerson, ChemBioChem 2009, 10, 1625–1629.

691. Synthesis of the Monomeric Unit of Lomaiviticin Aglycon, K.C. Nicolaou, A.L. Nold, H. Li, Angew. Chem. Int. Ed. 2009, 48, 5860–5963.

692. Total Synthesis and Biological Evaluation of Cortistatins A and J and Analogues Thereof, K.C. Nicolaou, X.-S. Peng, Y.P. Sun, D. Ploet, B. Zou, C. S. Lim, D.Y.-K. Chen, J. Am. Chem. Soc. 2009, 131, 10587–10597.

693. The True Structures of the Vannusals, Part 1: Initial Forays into Suspected Structures and Intelligence Gathering, K.C. Nicolaou, H. Zhang, A. Ortiz, Angew. Chem. Int. Ed. 2009, 48, 5642–5647.

694. The True Structures of the Vannusals, Part 2: Total Synthesis and Revised Structure of Vannusal B, K.C. Nicolaou, A. Ortiz, H. Zhang, Angew. Chem. Int. Ed. 2009, 48, 5648–5652.

695. Total Synthesis of Hirsutellone B, K.C. Nicolaou, D. Sarlah, T.R. Wu, W. Zhan, Angew. Chem. Int. Ed. 2009, 48, 6870–6874.

696. Rhodium-Catalyzed Asymmetric Enyne Isomerization of Terminal Alkynes and Formal Total Synthesis of (–)-Platensimycin, K.C. Nicolaou, A. Li, S.P. Ellery, D.J. Edmonds, Angew. Chem. Int. Ed. 2009, 48, 6293–6295.

697. Samarium Diiodide-Mediated Reactions in Total Synthesis, K.C. Nicolaou, S.P. Ellery, J.S. Chen, Angew. Chem. Int. Ed. 2009, 48, 7140–7165.

698. Total Synthesis of (+)-Haplophytine, K.C. Nicolaou, S.M. Dalby, S. Li, T. Suzuki, D.Y.-K. Chen, Angew. Chem. Int. Ed. 2009, 48, 7616–7620.

699. The Art of Total Synthesis Through Cascade Reactions, K.C. Nicolaou, J.S. Chen, Chem. Soc. Rev. 2009, 38, 2993–3009.

700. The β-D-Glucose Scaffold as a b-Turn Mimetic, R.F. Hirschmann, K.C. Nicolaou, A.R. Angeles, J.S. Chen, A.B. Smith, III, Acc. Chem. Res. 2009, 42, 1511–1520.

701. Identification of a Novel Small Molecule HIF-1a Translation Inhibitor, T. Narita, S. Yin, C.F. Gelin, C.S. Moreno, M. Yepes, K.C. Nicolaou, E.G. Van Meir, Clin. Cancer Res. 2009, 15, 6128–6136.

702. Total Synthesis and Biological Evaluation of (+)- and (–)-Bisanthraquinone Antibiotic BE-43472B and Related Compounds, K.C. Nicolaou, J. Becker, Y.H. Lim, A. Lemire, T. Neubauer, A. Montero, J. Am. Chem. Soc. 2009, 131, 14812–14826.

703. Total Syntheses of (±)-Platencin and (–)-Platencin, K.C. Nicolaou, G.S. Tria, D.J. Edmonds, M. Kar, J. Am. Chem. Soc. 2009, 131, 15909–15917.

704. Identification of Distinct Thiopeptide-Antibiotic Precursor Lead Compounds Using Translation Machinery Assays, A.L. Starosta, H. Qin, A. Mikolajka, G.Y.C. Leung, K. Schwinghammer, K.C. Nicoloau, D.Y.-K. Chen, B.S. Cooperman, D.N. Wilson, Chem. Biol. 2009, 16, 1087–1096.

705. Total Synthesis of Platensimycin and Related Natural Products, K.C. Nicolaou, A. Li, D.J. Edmonds, G.S. Tria, S.P. Ellery, J. Am. Chem. Soc. 2009, 131, 16905–16918.

706. Cortistatin A Is a High-Affinity Ligand of Protein Kinases ROCK, CDK8, and CDK11, V.J. Cee, D.Y.-K. Chen, M.R. Lee, K.C. Nicolaou, Angew. Chem. Int. Ed. 2009, 47, 8952–8957.

top

 

 

 

Publications

2010–Present

2000–2009

1990–1999

1980–1989

1970–1979


Patents

kcn image