隐藻素1的卤代醇类似物：合成与生物活性

Halohydrin analogues of cryptophycin 1: synthesis and biological activity.

作者信息

Georg G I, Ali S M, Stella V J, Waugh W N, Himes R H

机构信息

Department of Medicinal Chemistry, University of Kansas, Lawrence 66045, USA.

出版信息

Bioorg Med Chem Lett. 1998 Aug 4;8(15):1959-62. doi: 10.1016/s0960-894x(98)00356-4.

DOI:10.1016/s0960-894x(98)00356-4

PMID:9873466

Abstract

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.

摘要

抗有丝分裂药物隐藻素1的氯代、溴代和碘代衍生物2 - 4通过环氧环开环反应合成。这些化合物的生物活性在体外微管组装和细胞增殖试验中进行了测试。氯代衍生物2在微管蛋白试验中的活性低于3和4，但它们在增殖试验中均表现出相似的抑制作用。