Design and total synthesis of a superior family of epothilone analogues, which eliminate xenograft tumors to a nonrelapsable state

被引：58

作者：

Chou, TC

Dong, HJ

Rivkin, A

Yoshimura, F

Gabarda, AE

Cho, YS

Tong, WP

Danishefsky, SJ

机构：

[1] Mem Sloan Kettering Canc Ctr, Lab Bioorgan Chem, New York, NY 10021 USA

[2] Columbia Univ, Dept Chem, New York, NY 10027 USA

[3] Sloan Kettering Inst Canc Res, New York, NY 10021 USA

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2003年 / 42卷 / 39期

关键词：

antitumor agents; conformation analysis; epothilones; natural products; structure-activity relationships;

D O I：

10.1002/anie.200352361

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Unusually promising profiles of antitumor activity are displayed by 26-trifluoro-(E)-9,10-dehydro-dEpoB (1), the design and practical total synthesis of which is described. This compound promotes tumor shrinkage and disappearance in human xenografts in nude mice at well-tolerated doses, with complete remission for over two months and early rapid recovery of body weight to the pretreatment control levels.

引用

页码：4761 / 4767

页数：7

共 29 条

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