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期刊论文

DNA Cleavage Potency, Cytotoxicity, and Mechanism of Action of a Novel Class of Enediyne Prodrugs

戴伟民Wei-Min Dai*† Kwong Wah Lai† Anxin Wu† Wataru Hamaguchi† Mavis Yuk Ha Lee† Ling Zhou‡ Atsushi Ishii‡ and Sei-ichi Nishimoto‡

J. Med. Chem. 2002, 45, 758-761,-0001,():

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摘要/描述

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. LCMS analysis of the incubation mixture (pH 8.5, 37℃) 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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