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Design and Synthesis of C6−C8 Bridged Epothilone A

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posted on 2008-04-17, 00:00 authored by Weiqiang Zhan, Yi Jiang, Peggy J. Brodie, David G. I. Kingston, Dennis C. Liotta, James P. Snyder
A conformationally restrained epothilone A analogue (3) with a short bridge between methyl groups at C6 and C8 was designed and synthesized. Preliminary biological evaluation indicates 3 to be only weakly active (IC50 = 8.5 μM) against the A2780 human ovarian cancer cell line.

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Design and Synthesis of C6−C8 Bridged Epothilone A
Organic LettersOrganic Letters

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C 8EpothiloneC 6IC 50Bridgedanaloguemethyl groupsepothilonecancer cell linePreliminaryevaluationSynthesi8.5 μ Mconformationally

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