title: Synthesis of novel 4,6-disubstituted quinazoline derivatives, their anti-inflammatory and anti-cancer activity (cytotoxic) against U937 leukemia cell lines.
abstract: In view of the link between use of NSAIDs and altered cancer incidence and a growing evidence of COX-II implication in angiogenesis, a novel series of 4,6-disubstituted quinazoline derivatives have been synthesized starting from anthranilic acid derivatives 1 through conventional methods. Initially acylation followed by cyclisation to obtain benz-oxazinones 2 which on further treatment with ammonia yielded the crucial intermediate, 2-substituted benzamide (3). The products were subsequently cyclised to obtain quinazolones 4, chlorinated 5, then hooked to various optically pure alpha-amino acids to have 4,6-disubstituted quinazoline derivatives 6. All the derivatives 6 are screened for anti-inflammatory and anti-cancer activity against U937 leukemia cell lines. Some of the compounds exhibited promising anti-cancer activity with reference to standard drug Etoposide.
authors: Medicinal Chemistry Research Division, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506009, Andhrapradesh, India.
authors: P Mani
authors: PM
authors: Chandrika
authors: T
authors: T
authors: Yakaiah
authors: A Raghu Ram
authors: AR
authors: Rao
authors: B
authors: B
authors: Narsaiah
authors: N Chakra
authors: NC
authors: Reddy
authors: V
authors: V
authors: Sridhar
authors: J Venkateshwara
authors: JV
authors: Rao
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002351:Carrageenan; D049109:Cell Proliferation / Q000187:drug effects; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D006801:Humans; D008297:Male; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D020298:U937 Cells / Q000187:drug effects
chemical_list: D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D011799:Quinazolines; D002351:Carrageenan