新型噻唑萘二甲酰亚胺作为高效抗肿瘤和DNA光裂解剂：嵌入、侧链和取代基的影响

Novel thiazonaphthalimides as efficient antitumor and DNA photocleaving agents: effects of intercalation, side chains, and substituent groups.

作者信息

Li Zhigang, Yang Qing, Qian Xuhong

机构信息

State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116012, China.

出版信息

Bioorg Med Chem. 2005 Aug 15;13(16):4864-70. doi: 10.1016/j.bmc.2005.05.006.

DOI:10.1016/j.bmc.2005.05.006

PMID:15925513

Abstract

A series of novel antitumor and DNA photocleaving agents was designed and synthesized by fusing a (substituted) thiazole ring to the naphthalimide skeletons. C1, the most active compound against A549, was about 30-fold more cytotoxic than the compound amonafide. A1, the most active compound against P388, was about 6-fold more cytotoxic than amonafide. C2, the most efficient DNA intercalator, showed the strongest DNA photocleaving activity via superoxide anion produced under UV light at 360 nm.

摘要

通过将（取代的）噻唑环与萘二甲酰亚胺骨架融合，设计并合成了一系列新型抗肿瘤和DNA光裂解剂。对A549活性最高的化合物C1，其细胞毒性比氨茴酸酰胺大约高30倍。对P388活性最高的化合物A1，其细胞毒性比氨茴酸酰胺大约高6倍。最有效的DNA嵌入剂C2，在360nm紫外光下通过产生超氧阴离子显示出最强的DNA光裂解活性。