Variation der Ringgröße von Epothilonen – Totalsynthese von [14]-, [15]-, [17]- und [18]Epothilon A
K. C. Nicolaou
Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469
Search for more papers by this authorFrancisco Sarabia
Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469
Search for more papers by this authorSacha Ninkovic
Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469
Search for more papers by this authorM. Ray V. Finlay
Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469
Search for more papers by this authorChristopher N. C. Boddy
Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469
Search for more papers by this authorK. C. Nicolaou
Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469
Search for more papers by this authorFrancisco Sarabia
Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469
Search for more papers by this authorSacha Ninkovic
Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469
Search for more papers by this authorM. Ray V. Finlay
Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469
Search for more papers by this authorChristopher N. C. Boddy
Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469
Search for more papers by this authorAbstract
Kaum tolerant gegenüber Änderungen der Ringgröße ist das Pharmakophor des Epothilons A: Die 14-, 15-, 17- und 18gliedrigen Ringanaloga 1 (n = 1, 2, 4 bzw. 5) von Epothilon A und deren Desoxy-Verbindungen weisen im Tubulin-Polymerisations-Assay mit Ausnahme von [18]Desoxyepothilon A nur geringe Aktivitäten auf. Dies unterstreicht einmal mehr die hohe Spezifität des Tubulin-Rezeptors.
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