Synthesis, anti-inflammatory, and anticancer activity evaluation of some heterocyclic amidine and bis-amidine derivatives

✍ Scribed by Sham M. Sondhi; Reshma Rani; Partha Roy; S. K. Agrawal; A. K. Saxena

• Publisher: Journal of Heterocyclic Chemistry
• Year: 2011
• Tongue: English
• Weight: 117 KB
• Volume: 48
• Category: Article
• ISSN: 0022-152X
• DOI: 10.1002/jhet.658

✦ Synopsis

Abstract

Heterocyclic amidine derivatives of benzothiazole (6a, 6b, 6c), benzimidazole (6d, 6e, 6f), benzoxazole (6g, 6h, 6i), and bis‐amidine derivatives of pyrimidine, (7a, 7b) & triazole (7c, 7d, 7e) ring system have been synthesized by nucleophilic addition reaction. All these compounds were screened for anti‐inflammatory and anticancer activities. At a dose of 50 mg/kg p.o., compounds 6c (39%), 6e (39%), and 6f (39%) exhibited anti‐inflammatory activity comparable to standard drug ibuprofen, which showed 39% activity and compounds 6b, 6e, 7a, and 7c exhibited moderate anticancer activity against cervix (HELA); neuroblastoma (IMR‐32); breast (MCF‐7), leukemia (THP‐1); and cervix (HELA) human cancer cell lines, respectively. J. Heterocyclic Chem., (2011).