Antimitotic activities of 2-phenylindole-3-carbaldehydes in human breast cancer cells

被引：76

作者：

Kaufmann, Doris ^{[1
]}

Pojarova, Michaela ^{[1
]}

Vogel, Susanne ^{[1
]}

Liebl, Renate ^{[1
]}

Gastpar, Robert ^{[1
]}

Gross, Dietmar ^{[1
]}

Nishino, Tsuyuki ^{[1
]}

Pfaller, Tobias ^{[1
]}

von Angerer, Erwin ^{[1
]}

机构：

[1] Univ Regensburg, Inst Pharm, D-93040 Regensburg, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 15期

关键词：

phenylindoles; breast cancer; tubulin polymerization; cell cycle arrest;

D O I：

10.1016/j.bmc.2007.05.030

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Small molecules such as indoles are attractive as inhibitors of tubulin polymerization. Thus a number of 2-phenylindole-3-carbaldehydes with lipophilic substituents in both aromatic rings was synthesized and evaluated for antitumor activity in MDA-MB 231 and MCF-7 breast cancer cells. Some 5-alkylindole derivatives with a 4-methoxy group in the 2-phenyl ring strongly inhibit the growth of breast cancer cells with IC50 values of 5-20 nM. Their action can be rationalized by the cell cycle arrest in G(2)/M phase due to the inhibition of tubulin polymerization. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：5122 / 5136

页数：15

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