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Synthesis and Antileukemic Activity of 1-((S)-2-Amino-4,5,6,7-tetrahydrobenzo[d]thiazol-6-yl)-3-(substituted phenyl)urea Derivatives

Prasanna, Doddakunche S and Kavitha, Chandagirikoppal V and Vinaya, Kambappa and Ranganatha, Somasagara R and Raghava, Byregowda and Kumar, Yelekere Sunil C and Raghavan, Sathees C and Rangappa, Kanchugarakoppal S (2010) Synthesis and Antileukemic Activity of 1-((S)-2-Amino-4,5,6,7-tetrahydrobenzo[d]thiazol-6-yl)-3-(substituted phenyl)urea Derivatives. In: Bulletin of the Chemical Society of Japan, 83 (6). pp. 689-697.

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Official URL: http://www.jstage.jst.go.jp/article/bcsj/83/6/83_6...

Abstract

Heterocyclic urea derivatives play an important role as anticancer agents because of their good inhibitory activity against receptor tyrosine kinases (RTKs), raf kinases, protein tyrosine kinases (PTKs), and NADH oxidase, which play critical roles in many aspects of tumorigenesis. Benzothiazole moiety constitutes an important scaffold of drugs, possessing several pharmacological functions, mainly the anticancer activity. Based on these interesting properties of benzothiazoles and urea moiety to obtain new biologically active agents, we synthesized a series of novel 1-((S)-2-amino-4,5,6.7-tetrahydrobenzo[d]thiazol-6-yl)-3-(substituted phenyl)urea derivatives and evaluated for their efficacy as antileukemic agents against two human leukemic cell lines (K562 and Reh). These compounds showed good and moderate cytotoxic effect to cancer cell lines tested. Compounds with electron-withdrawing chloro and fluoro substituents on phenyl ring showed good activity and compounds with electron-donating methoxy group showed moderate activity. Compound with electron-withdrawing dichloro substitution on phenyl ring of aryl urea showed good activity. Further, lactate dehydrogenase (LDH) assay, flow cytometric analysis of annexin V-FITC/propidium iodide (PI) double staining and DNA fragmentation studies showed that compound with dichloro substitution on phenyl ring of aryl urea can induce apoptosis.

Item Type: Journal Article
Additional Information: Copyright of this article belongs to Chemical Society of Japan.
Department/Centre: Division of Biological Sciences > Biochemistry
Date Deposited: 11 Aug 2010 08:10
Last Modified: 11 Aug 2010 08:10
URI: http://eprints.iisc.ernet.in/id/eprint/31223

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