Synthesis, anticancer activity and docking of some substituted benzothiazoles as tyrosine kinase inhibitors

H.A. Bhuva, S.G. Kini

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71 Citations (Scopus)

Abstract

Protein tyrosine kinases occupy a central position in the control of cellular proliferation and its inactivation might lead to the discovery of a new generation anticancer compounds. Substituted benzothiazoles have been found to mimic the ATP-competitive binding of genistein and quercetin to tyrosine kinase. A series of novel 2-phenyl-1,3-benzothiazoles were synthesized and characterised by IR, 1H NMR and mass spectroscopy. All the compounds were tested for their anticancer activity against MCF-7 breast cancer cell line with the MTT assay. Most of the compounds showed moderate to good anti-breast cancer activity. Anticancer activity varied with substitution on the benzothiazole nucleus with halogens and at 4 position, substitution of the 2-phenyl moiety with methyl and methoxy groups was also explored. Among the compounds tested with MTT assay, mono fluoro substitution on benzothiazole nucleus and 4'-methyl variations at 2-phenyl position demonstrated highest percent growth inhibition of MCF-7 cells. Docking studies of the synthesised compounds was done on EGFR using GRIP batch docking method to study their observed activity. © 2010 Elsevier Inc.
Original languageEnglish
Pages (from-to)32-37
Number of pages6
JournalJournal of Molecular Graphics and Modelling
Volume29
Issue number1
DOIs
Publication statusPublished - 2010

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