Sondhi, Sham M. and Rani, Reshma and Gupta, P. P. and Agrawal, S. K. and Saxena, A. K. (2009) Synthesis, anticancer, and anti-inflammatory activity evaluation of methanesulfonamide and amidine derivatives of 3,4-diaryl-2-imino-4-thiazolines. Molecular Diversity, 13 (3). pp. 357-366. ISSN 1381-1991

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Condensation of 3,4-diaryl-2-imino-4-thiazolines 1a–j with methanesulfonyl chloride gavemethanesulfonamide derivatives 2a–j. Condensation of 2-cyanopyrazine,4-cyanopyridine, and 2-cyanopyridine with 3,4-diaryl-2-imino-4-thiazolines 1h–m in the presence of sodium methoxide afforded amidine derivatives 3a–j. Compounds 2a–j and 3a–j were screened against various human cancer cell lines(COLO-205, HEP-2, A-549, IMR-32) and their percentage growth inhibition profile determined at 1 × 10−5M. The antiinflammatory activity of these compoundswas assessed using the carrageenan-induced paw edema model. Compound 2i exhibited 34.7% anti-inflammatory activity at 50 mg/kg p.o.,which is comparable to standard care drug phenyl butazone (37% activity at 50 mg/kg p.o.)

Item Type: Article
Subjects: Chemical Sciences
Pharmacological Sciences
Depositing User: Mr. Amit Nargotra
Date Deposited: 03 Jan 2012 05:20
Last Modified: 03 Jan 2012 05:20

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