title: Synthesis of Novel Pyrido[1,2-a]pyrimidine-3-carboxamide Derivatives and Their Anticancer Activity.
abstract: A series of novel pyrido[1,2-a]pyrimidine-3-carboxamide derivatives 6a-n were prepared starting from 2(1H) pyridone 1 via hydrolysis, de-carboxylation, selective O-alkylation followed by rearrangement to give pyridine-2-amine 3. Compound 3 on reaction with ethoxy methylene malonic diethyl ester (EMME) under a conventional method followed by cyclization under micro wave irradiation (MWI) conditions resulted in product 5. Compound 5 on coupling with diverse substituted aliphatic amines formed title compounds 6a-n. All the products 6a-n were screened against four human cancer cell lines and compounds 6h-k and n which showed promising anticancer activity have been identified.
authors.affiliation: Fluoroorganic Division, Indian Institute of Chemical Technology.
authors.forename: Gautham
authors.initials: G
authors.lastname: Santhosh Kumar
authors.forename: Gaddameedi
authors.initials: G
authors.lastname: Jitender Dev
authors.forename: Nagiri
authors.initials: N
authors.lastname: Ravi Kumar
authors.forename: Desireddy
authors.initials: D
authors.lastname: Krishna Swaroop
authors.forename: Yedla
authors.initials: Y
authors.lastname: Poorna Chandra
authors.forename: Chityala
authors.initials: C
authors.lastname: Ganesh Kumar
authors.forename: Banda
authors.initials: B
authors.lastname: Narsaiah
mesh_terms: D000478:Alkylation; D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D003500:Cyclization; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D011743:Pyrimidines