DNA-cleavage studies on N-substituted monocyclic enediynes:: Enhancement of potency by incorporation of intercalating or electron poor aromatic ring and subsequent design of a novel phototriggerable acyclic enediyne

被引:49
作者
Basak, A [1 ]
Bdour, HM [1 ]
Shain, JC [1 ]
Mandal, S [1 ]
Rudra, KR [1 ]
Nag, S [1 ]
机构
[1] Indian Inst Technol, Dept Chem, Kharagpur, W Bengal, India
关键词
D O I
10.1016/S0960-894X(00)00237-7
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
A number of novel N-substituted enediynes (azaenediynes) 1-4 were synthesized as DNA cleaving agents. Enhancement of DNA cleavage potency was observed with those compounds which could interact with DNA through intercalation of the extended aromatic ring or through electrostatic attraction with electron poor aromatic ring. An acyclic enediyne 5 with a novel phototriggerable device was also synthesized and its DNA-cleaving activity was established. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1321 / 1325
页数:5
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