Halohydrin analogues of cryptophycin 1: Synthesis and biological activity

被引：30

作者：

Georg, GI ^{[1
]}

Ali, SM

Stella, VJ

Waugh, WN

Himes, RH

机构：

[1] Univ Kansas, Dept Med Chem, Lawrence, KS 66045 USA

[2] Univ Kansas, Dept Pharmaceut Chem, Lawrence, KS 66045 USA

[3] Univ Kansas, Dept Biochem & Mol Cell Biol, Lawrence, KS 66045 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(98)00356-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The chloro-, bromo-, and iodo-derivatives 2-4 of the antimitotic drug cryptophycin 1 were synthesized by opening the epoxide ring. The biological activities of the compounds were tested in an in vitro microtubule assembly and a cell proliferation assay. The chloro-derivative 2 showed lower activity in the tubulin assay compared to 3 and 4, but they all showed similar inhibition in the proliferation assay. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1959 / 1962

页数：4

共 16 条

[1] NUCLEOPHILIC CATALYSIS IN THE INSERTION OF SILICON HALIDES INTO OXIRANES - A SYNTHESIS OF ORTHO-PROTECTED VICINAL HALOHYDRINS [J].