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Synthesis and Identification of a new class of antileukemic agents containing 2-(arylcarboxamide)-(S)-6-amino-4,5,6,7-tetrahydrobenzod]thiazole

Prasanna, DS and Kavitha, CV and Vinaya, K and Ranganatha, SR and Raghavan, Sathees C and Rangappa, KS (2010) Synthesis and Identification of a new class of antileukemic agents containing 2-(arylcarboxamide)-(S)-6-amino-4,5,6,7-tetrahydrobenzod]thiazole. In: European Journal of Medicinal Chemistry, 45 (11). pp. 5331-5336.

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Official URL: http://dx.doi.org/10.1016/j.ejmech.2010.08.056


Recently we have reported the effect of (S)-6-aryl urea/thiourea substituted-2-amino-4,5,6,7-tetrahydrobenzod]thiazole derivatives as potent anti-leukemic agents. To elucidate further the Structure Activity Relationship (SAR) studies on the anti-leukemic activity of (S)-2,6-diamino-4,5,6,7 tetrahydrobenzod]thiazole moiety, a series of 2-arlycarboxamide substituted-(S)-6-amino-4,5,6,7-tetrahydrobenzod]thiazole were designed, synthesized and evaluated for their anti-leukemic activity by trypan blue exclusion, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), lactate dehydrogenase (LDH) assays and cell cycle analysis. Results suggest that the position, number and bulkiness of the substituent on the phenyl ring of aryl carboxamide moiety at 2nd position of 6-amino-4,5,6,7-tetrhydrobenzod]thiazole play a key role in inhibiting the proliferation of leukemia cells. Compounds with ortho substitution showed poor activity and with meta and para substitution showed good activity. (C) 2010 Elsevier Masson SAS. All rights reserved.

Item Type: Journal Article
Publication: European Journal of Medicinal Chemistry
Publisher: Elsevier Science
Additional Information: Copyright of this article belongs to Elsevier Science.
Keywords: Tetrahydrobenzod]thiazole; Cytotoxicity; Apoptosis; Cancer therapeutics; Leukemia
Department/Centre: Division of Biological Sciences > Biochemistry
Date Deposited: 23 Dec 2010 10:14
Last Modified: 23 Dec 2010 10:14
URI: http://eprints.iisc.ac.in/id/eprint/34328

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