3-substituted 7-phenyl-pyrroloquinolinones show potent cytotoxic activity in human cancer cell lines

被引：43
作者：
Gasparotto, Venusia
Castagliuolo, Ignazio
Ferlin, Maria Grazia
机构：
[1] Univ Padua, Sch Pharm, Dept Pharmaceut Sci, I-35131 Padua, Italy
[2] Univ Padua, Sch Pharm, Dept Histol Microbiol & Med Biotechnol, I-35131 Padua, Italy
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 22期
关键词：
D O I：
10.1021/jm070534b
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel series of 3-alkyl-substituted 7-phenyl-3H-pyrrolo[3,2-jlquinolin-9-ones (7-PPyQs) was synthesized with the aim to optimize the cytotoxic activity of recently identified PPyQs, promising inhibitors of tubulin polymerization. All compounds inhibited the growth of 11 human tumor cell lines at submicromolar concentrations as well as two human resistant cancer sublines, A549-T12 and A549-T24. FACS analysis indicated that all compounds caused significant arrest of the A549 cell cycle in G(2)/M phase at 0.1 and 1 mu M and a good correlation between the cytotoxicity IC50 and their ability to block the cell cycle was observed.
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收藏
页码：5509 / 5513
页数：5
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