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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Preliminary In-Vitro Cytotoxic Activity of Novel Substituted diaryl-imidazo [2,1,b]-benzothiazole Derivatives

Author(s): Jitender K. Malik, Malleshappa N. Noolvi, Fakkirappa V. Manvi, B.K. Nanjwade, Harun M. Patel, Manjula S. N., Mallikarjuna Rao C. and Ashutosh Barve

Volume 8 , Issue 8 , 2011

Page: [717 - 724] Pages: 8

DOI: 10.2174/157018011796576015

Price: $65

Abstract

A novel series of substituted diaryl imidazo[2,1-b]benzothiazole derivatives (8a-y) were synthesized by condensation reaction between 2-amino benzothiazole derivatives (3a-g) and substituted α-bromo-1, 2-(substituted) diaryl-1- ethanones (7a-i). The structures of the synthesized compounds were established by IR, 1H NMR, 13C NMR and mass spectroscopical data. The compounds (8a-y) were evaluated for their in-vitro cytotoxic activity on murine (B16F10) and human (MCF-7) cancer cells by using MTT assay. From the in vitro studies compounds 8p, 8u and 8y were found most effective with an IC50 range of 0.56 -27.50 µ M in MCF-7 and 2.57-36.54 µ M in B16F10 cells.

Keywords: Diaryl imidazo[2,1-b]benzothiazole, MTT assay, DNA damage, MCF-7, diaryl-1-ethanones, 1H NMR, Mass spectroscopical data, cancer, molecular anatomy, benzothiazole, aryl hydrocarbon receptor (AhR), melanoma, leismaniacidal, orthophosphoric acid


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