Design, synthesis, and evaluation of novel 6-chloro-/fluorochromone derivatives as potential topoisomerase inhibitor anticancer agents

被引：89

作者：

Ishar, MPS ^{[1
]}

Singh, G

Singh, S

Sreenivasan, KK

Singh, G

机构：

[1] Guru Nanak Dev Univ, Dept Pharmaceut Sci, Amritsar 143005, Punjab, India

[2] Manipal Coll Pharmaceut Sci, Dept Pharmaceut Chem, Manipal 576104, Karnataka, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 05期

关键词：

anticancer; antitumor; DNA topoisomerases; topoisomerase inhibitors; chromone;

D O I：

10.1016/j.bmcl.2005.11.044

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

6-Chloro-2-pyrrolidino-/morpholino-/piperidino-/N-methylpiperazino-3-formyl-chromones (13-16) and 6-fluoro-2,7-dimorpholino-/piperidino-/N-methylpiperazino-3-formylchromones (17-19) have been synthesized as potential topoisomerase inhibitor anticancer agents, and evaluated, in vitro, against Ehrlich ascites carcinoma (EAC) cells, and also in vivo on EAC bearing mice. The compounds displayed promising anticancer activity under these test systems and shall serve as useful 'leads' for further design. (C) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1366 / 1370

页数：5

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