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Eur J Med Chem. 2012 Oct;56:166-78. doi: 10.1016/j.ejmech.2012.08.021. Epub 2012 Aug 23.

Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.

Author information

1
Division of Organic Chemistry, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 607, India. ahmedkamal@iict.res.in

Abstract

A series of combretastatin-amidobenzothiazole conjugates have been synthesized and evaluated for their anticancer activity. All these compounds exhibited significant anticancer activity and the most potent compound (11a) showed GI(50) values ranging 0.019-11 μM. Biological studies such as cell cycle distribution, effect on tubulin polymerization and effect on ERK signalling pathway have been examined in MCF-7 cell line. FACS analysis revealed that these compounds induced cell cycle arrest at G2/M phase. Compound 11a showed significant effect on tubulin polymerization and affected the ERK signalling pathway that result in the decreased levels of ERK1/2, p-ERK and c-Jun proteins. Docking experiments have shown that the active molecules interact and bind well in the ATP binding pocket of ERK protein.

PMID:
22982122
DOI:
10.1016/j.ejmech.2012.08.021
[Indexed for MEDLINE]

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