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Synthesis and cytotoxic activity of novel 10-alkylated docetaxel analogs.

作者信息

Nakayama K, Terasawa H, Mitsui I, Ohsuki S, Uoto K, Iimura S, Soga T

机构信息

New Product Research Laboratories IV, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.

出版信息

Bioorg Med Chem Lett. 1998 Mar 3;8(5):427-32. doi: 10.1016/s0960-894x(98)00040-7.

Abstract

An alkylation method of docetaxel at the C-10 position has been established by a radical coupling reaction using a 10-xanthate derivative of 7-O-TES-10-deacetylbaccatin III and appropriate alkenes. In addition the cytotoxic activity of 10-alkylated docetaxel analogs was evaluated. Among these analogs, a derivative having a methoxycarbonyl group at the end of the alkyl moiety exhibited more potent cytotoxic activity than docetaxel.

摘要

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