Synthesis and biological evaluation of highly potent analogues of epothilones B and D

被引：60

作者：

Altmann, KH ^{[1
]}

Bold, G ^{[1
]}

Caravatti, G ^{[1
]}

Flörsheimer, A ^{[1
]}

Guagnano, V ^{[1
]}

Wartmann, M ^{[1
]}

机构：

[1] Novartis Pharma AG, TA Oncol Res, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(00)00555-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new epothilone B and D analogues incorporating fused hetero-aromatic side chains have been prepared. The synthetic strategy is based on olefin 3 as the common intermediate and allows variation of the side-chain structure in a highly convergent and stereoselective manner. Epothilone analogues 1a-d and 2a-d are more potent inhibitors of cancer cell proliferation than the corresponding parent epothilones B or D. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2765 / 2768

页数：4

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