Antimitotic activities of 2-phenylindole-3-carbaldehydes in human breast cancer cells |
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Authors: | Kaufmann Doris Pojarová Michaela Vogel Susanne Liebl Renate Gastpar Robert Gross Dietmar Nishino Tsuyuki Pfaller Tobias von Angerer Erwin |
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Institution: | Institut für Pharmazie, Universität Regensburg, D-93040 Regensburg, Germany |
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Abstract: | 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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