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Antimitotic activities of 2-phenylindole-3-carbaldehydes in human breast cancer cells. 2007
Doris Kaufmann, and
Michaela Pojarová, and
Susanne Vogel, and
Renate Liebl, and
Robert Gastpar, and
Dietmar Gross, and
Tsuyuki Nishino, and
Tobias Pfaller, and
Erwin von Angerer
Institut für Pharmazie, Universität Regensburg, Regensburg, Germany.
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 IC(50) values of 5-20nM. Their action can be rationalized by the cell cycle arrest in G(2)/M phase due to the inhibition of tubulin polymerization.
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