A Total Synthesis of Epothilones Using Solid??Supported Reagents and Scavengers

RI Storer, T Takemoto, PS Jackson…

Index: Storer, R. Ian; Takemoto, Toshiyasu; Jackson, Philip S.; Ley, Steven V. Angewandte Chemie - International Edition, 2003 , vol. 42, # 22 p. 2521 - 2525

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Citation Number: 62

Abstract

The epothilone natural products [1] exhibit extraordinary cytotoxic biological activity by promoting GTP-independent tubulin polymerization. This mode of action inhibits the growth of tumors by inducing mitotic arrest, followed by cell apoptosis. Mechanistic investigations have revealed that the epothilones bind competitively to the same, or overlapping, sites in b- tubulin as taxol.[2] However, certain epothilones exhibit a higher activity than taxol, even ...

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