Halogenated 2-amino-4H-pyrano[3,2-h]quinoline-3-carbonitriles as antitumor agents and structure–activity relationships of the 4-, 6-, and 9-positions

被引：0

作者：

Ahmed M. Fouda

机构：

[1] King Khalid University,Chemistry Department, Faculty of Science

来源：

Medicinal Chemistry Research | 2017年 / 26卷

关键词：

8-Hydroxyquinoline derivatives; 4; -Pyrano[3,2-; ]quinoline; Antitumor; Lipophilicity; SAR;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

A series of halogenated 2-amino-4-aryl-4H-pyrano[3,2-h]quinoline-3-carbonitrile derivatives were prepared via interaction of 8-hydroxyquinoline, 5-chloro-8-hydroxyquinoline, and 8-hydroxy-2-methylquinoline with various α-cyanocinnamonitriles. The assignments of the structure of all synthesized compounds were based on spectral data. The cytotoxic activities of the synthesized compounds against four human tumor cell lines MCF-7, HCT-116, HepG-2, and A549 in comparison with the reference drugs Vinblastine and Colchicine were determined by microculture tetrazolium assay. Several compounds showed significant cytotoxic activity. The structure–activity relationship studies reported that the substitution at 4-, 6-, and 9-positions in several 2-amino-4H-pyrano[3,2-h]quinoline nucleus with the specific halogen atom and lipophilicity increases the ability of the molecule against the different cell lines.

引用

页码：302 / 313

页数：11

共 41 条

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