DNA cleavage potency, cytotoxicity, and mechanism of action of a novel class of enediyne prodrugs
DNA cleavage potency, cytotoxicity, and mechanism of action of a novel class of enediyne prodrugs
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DOI：
10.1021/jm015588e
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发表时间：
2002-02-14
影响因子：
7.3
通讯作者：
Nishimoto, S
中科院分区：
文献类型：
--
作者：
Dai, WM;Lai, KW;Nishimoto, S
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.
