title: Microwave-assisted synthesis of pyrimido[4,5-b][1,6]naphthyridin-4(3H)-ones with potential antitumor activity.
abstract: The 6,7,8,9-tetrahydropyrimido[4,5-b][1,6]naphthyridin-4(3H,5H,10H)-ones 4,5a-g and their oxidized forms 6,7a-g were obtained from the catalyst-free reaction of 6-amino-2-methylthiopyrimidin-4(3H)-one 3 and (E)-3,5-bis(benzylidene)-1-alkyl-4-piperidones 1,2a-g under Microwave irradiation and their subsequent oxidation process with p-chloranil. Eighteen of the new compounds were evaluated in the US National Cancer Institute (NCI), where compound 4g presented a remarkable activity against 57 cancer cell lines, with the most important GI(50) values ranging from 1.48 to 9.92 μM from in vitro assays.
authors.affiliation: Grupo de Investigación de Compuestos Heterocíclicos, Departamento de Química, Universidad del Valle, AA 25360 Cali, Colombia. braulio.insuasty@correounivalle.edu.co
authors.forename: Braulio
authors.initials: B
authors.lastname: Insuasty
authors.forename: Diana
authors.initials: D
authors.lastname: Becerra
authors.forename: Jairo
authors.initials: J
authors.lastname: Quiroga
authors.forename: Rodrigo
authors.initials: R
authors.lastname: Abonia
authors.forename: Manuel
authors.initials: M
authors.lastname: Nogueras
authors.forename: Justo
authors.initials: J
authors.lastname: Cobo
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008872:Microwaves; D015394:Molecular Structure; D009287:Naphthyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009287:Naphthyridines; D011744:Pyrimidinones