Kaufmann, Doris and Pojarová, Michaela and Vogel, Susanne and Liebl, Renate and Gastpar, Robert and Gross, Dietmar and Nishino, Tsuyuki and Pfaller, Tobias and Angerer, Erwin von (2007) Antimitotic activities of 2-phenylindole-3-carbaldehydes in human breast cancer cells. Bioorganic & medicinal chemistry 15 (15), pp. 5122-36.
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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.
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)|
|Subjects:||500 Science > 570 Life sciences|
500 Science > 540 Chemistry & allied sciences
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Owner:||Prof. Armin Buschauer|
|Deposited On:||03 Dec 2008 15:29|
|Last Modified:||05 Aug 2009 13:48|