Total synthesis as a resource in the discovery of potentially valuable antitumor agents: Cycloproparadicicol

被引：69

作者：

Yamamoto, K

Garbaccio, RM

Stachel, SJ

Solit, DB

Chiosis, G

Rosen, N

Danishefsky, SJ

机构：

[1] Sloan Kettering Inst Canc Res, Bioorgan Chem Lab, New York, NY 10021 USA

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

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

[4] Sloan Kettering Inst Canc Res, Dept Med, New York, NY 10021 USA

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2003年 / 42卷 / 11期

关键词：

antitumor agents; chaperone proteins; natural products; structure-activity relationships; synthesis design;

D O I：

10.1002/anie.200390329

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A highly convergent synthesis was used to prepare a series of epimers and analogues of radicicol (1). Biological assessment revealed a previously unrecognized correlation between stereochemistry and antitumor potential in these compounds. Significantly, cycloproparadicicol (2) showed promising therapeutic properties based on inhibition of chaperones.

引用

页码：1280 / 1284

页数：5

共 36 条

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