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Chem Pharm Bull (Tokyo) ; 63(8): 584-90, 2015.
Article in English | MEDLINE | ID: mdl-26235166

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.


Subject(s)
Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Pyrimidines/chemistry , Pyrimidines/pharmacology , Alkylation , Amides/chemical synthesis , Amides/chemistry , Amides/pharmacology , Antineoplastic Agents/chemical synthesis , Cell Line, Tumor , Cyclization , Drug Screening Assays, Antitumor , Humans , Neoplasms/drug therapy , Pyrimidines/chemical synthesis , Structure-Activity Relationship
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