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Synthesis and Cytotoxic Evaluation of Novel 2-(4-(2,2,2-Trifluoroethoxy)-3-methylpyridin-2-ylthio)-1H-benzo[d]imid azole Derivatives

Ranganatha, SR and Kavitha, CV and Vinaya, K and Prasanna, DS and Chandrappa, S and Raghavan, Sathees C and Rangappa, KS (2009) Synthesis and Cytotoxic Evaluation of Novel 2-(4-(2,2,2-Trifluoroethoxy)-3-methylpyridin-2-ylthio)-1H-benzo[d]imid azole Derivatives. In: Archives of Pharmacal Research, 32 (10). pp. 1335-1343.

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Official URL: http://www.springerlink.com/content/d97w023941ltk0...

Abstract

The present work deals with the anticancer effect of benzimidazole derivatives associated with the pyridine framework. By varying the functional group at N-terminal of the benzimidazole by different L-amino acids, several 2-(4-(2,2,2-trifluoroethoxy)-3-methylpyridin-2-ylthio)-1H-benzo[d]imid azole derivatives 9(a-j) were synthesized. Their chemical structures were confirmed by H-1 NMR, IR and mass spectroscopic techniques. The synthesized compounds were examined for their antiproliferative effects against human leukemia cell lines, K562 and CEM. The preliminary results showed most of the derivatives had moderate antitumor activity. Compound 9j containing cysteine residue exhibited good inhibition compared to other amino acid resides. In addition DNA fragmentation results suggest that 9j is more cytotoxic and able to induce apoptosis.

Item Type: Journal Article
Additional Information: Copyright for this article belongs to Pharmaceutical Society of Korea.
Keywords: Benzimidazole; Amino acids; Cytotoxicity; Chronic myelogenous leukemia
Department/Centre: Division of Biological Sciences > Biochemistry
Depositing User: Id for Latest eprints
Date Deposited: 02 Dec 2009 05:14
Last Modified: 02 Dec 2009 05:16
URI: http://eprints.iisc.ac.in/id/eprint/24997

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