Synthesis and identification of a new class of antileukemic agents containing 2-(arylcarboxamide)-(S)-6-amino-4,5,6,7-tetrahydrobenzodthiazole

Prasanna, D. S. and Kavitha, C. V. and Vinaya, K. and Ranganatha, S. R. and Raghavan, Sathees C. and Rangappa, K. S. (2010) Synthesis and identification of a new class of antileukemic agents containing 2-(arylcarboxamide)-(S)-6-amino-4,5,6,7-tetrahydrobenzodthiazole. European Journal of Medicinal Chemistry, 45 (11). 5331 - 5336. ISSN 0223-5234

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Recently we have reported the effect of (S)-6-aryl urea/thiourea substituted-2-amino-4,5,6,7-tetrahydrobenzodthiazole 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-tetrahydrobenzodthiazole moiety, a series of 2-arlycarboxamide substituted–(S)-6-amino-4,5,6,7-tetrahydrobenzodthiazole 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-tetrhydrobenzodthiazole 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.

Item Type: Article
Uncontrolled Keywords: Tetrahydrobenzodthiazole, Cytotoxicity, Apoptosis, Cancer therapeutics, Leukemia
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: LA manjunath user
Date Deposited: 05 Jul 2019 07:31
Last Modified: 10 Dec 2019 09:30

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