化学
肿瘤细胞
结构-活动关系
计算生物学
组合化学
药理学
癌症研究
生物
生物化学
体外
作者
Maria de Fatima Pereira,Christophe Rochais,Patrick Dallemagne
出处
期刊:Anti-cancer Agents in Medicinal Chemistry
[Bentham Science]
日期:2015-09-02
卷期号:15 (9): 1080-1091
被引量:22
标识
DOI:10.2174/1871520615666150520143600
摘要
Phenanthroindolizidine and phenanthroquinolizidine derivatives constitute a series of compounds that are being intensively studied as potential anticancer agents. Related natural products such as antofine and tylophorine alkaloids are well known for their high cytotoxic activity; however, their clinical application has been limited because of their side effects. In this review we report, in detail, on the main structural modifications applied to the phenanthroindolizidine and phenanthroquinolizidine skeletons, and we also describe their associated anticancer activities. New derivatives with promising antitumoral activities have emerged. Simplified analogues were prepared using rapid synthetic routes, and a certain number of these analogues displayed increased anticancer activity and selectivity towards tumor cell lines. It is hoped that a better understanding of the mechanisms of action associated with structure-activity relationships (SAR) will enable us to rationalize the development of new anticancer drugs.
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