水溶性喜树碱衍生物，它们是内在的拓扑异构酶I毒物。

Water-soluble camptothecin derivatives that are intrinsic topoisomerase I poisons.

作者信息

Rahier Nicolas J, Eisenhauer Brian M, Gao Rong, Jones Shannon H, Hecht Sidney M

机构信息

Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA.

出版信息

Org Lett. 2004 Feb 5;6(3):321-4. doi: 10.1021/ol030119n.

DOI:10.1021/ol030119n

PMID:14748583

Abstract

[structure: see text] In an effort to improve the water solubility of camptothecin, four 20-O-phosphate and phosphonate analogues have been prepared. These analogues are freely water soluble, stable at physiological pH, and stabilize the human topoisomerase I-DNA covalent binary complex with the same sequence selectivity as camptothecin itself. All four compounds inhibited the growth of yeast expressing human topoisomerase I in an enzyme-dependent fashion.

摘要

[结构：见正文] 为了提高喜树碱的水溶性，已制备了四种20-O-磷酸酯和膦酸酯类似物。这些类似物可自由溶于水，在生理pH值下稳定，并以与喜树碱本身相同的序列选择性稳定人拓扑异构酶I-DNA共价二元复合物。所有四种化合物均以酶依赖性方式抑制表达人拓扑异构酶I的酵母的生长。