DNA cleavage potency, cytotoxicity, and mechanism of action of a novel class of enediyne prodrugs

被引：33

作者：

Dai, WM

Lai, KW

Wu, AX

Hamaguchi, W

Lee, MYH

Zhou, L

Ishii, A

Nishimoto, S

机构：

[1] Hong Kong Univ Sci & Technol, Dept Chem, Kowloon, Hong Kong, Peoples R China

[2] Kyoto Univ, Grad Sch Engn, Dept Energy & Hydrocarbon Chem, Sakyo Ku, Kyoto 6068501, Japan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 04期

关键词：

D O I：

10.1021/jm015588e

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have discovered a novel class of (E)-3-acyloxy-4-(arylmethylidene)cyclodeca-1,5-diynes which exhibit promising enediyne-like DNA cleavage and cytotoxic activities. LC-MS analysis of the incubation mixture (pH 8.5, 37 degreesC) confirmed formation of 10-membered ring enediyne presumably via an allylic cation and suggested that the 1,4-benzenoid diradical might be one of the active species for DNA damage and cytotoxicity.

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页码：758 / 761

页数：4

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