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

Abstract

Figure represented. Heterocyclic amidine derivatives of benzothiazole (6a-c), benzimidazole (6d-f), benzoxazole (6g-i), and bis-amidine derivatives of pyrimidine, (7a, 7b) & triazole (7c-e) 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. © 2011 HeteroCorporation.