title: Quinolinyl and quinolinyl N-oxide chalcones: synthesis, antifungal and cytotoxic activities.
abstract: A series of new 6-quinolinyl and quinolinyl N-oxide chalcones were efficiently prepared. All chalcones were tested by minimal inhibitory concentration (MIC) against three species of Candida, Cryptococcus gattii and Paracoccidioides brasiliensis. The effect of these compounds was also tested on the survival and growth of the human cancer cell lines UACC-62 (melanoma), MCF-7 (breast), TK-10 (renal) and leukemic cells, Jurkat and HL60. The compounds tested presented strong activity against P. brasiliensis, most importantly compound 4e. C. gattii also presented interesting susceptibility for compounds 5b and 5f. The cytotoxic activity showed that compounds 3c and 4e, presented the best activity against MCF-7 and TK-10. For leukemic cells the compounds 4f, 3g, 4g and 5g have shown the best activity.
authors.affiliation: Departamento de Química, Universidade Federal de Santa Catarina, Florianópolis, SC, Brazil.
authors.forename: Luciana
authors.initials: L
authors.lastname: de Carvalho Tavares
authors.forename: Susana
authors.initials: S
authors.lastname: Johann
authors.forename: Tânia
authors.initials: T
authors.lastname: Maria de Almeida Alves
authors.forename: Juliana Correia
authors.initials: JC
authors.lastname: Guerra
authors.forename: Elaine
authors.initials: E
authors.lastname: Maria de Souza-Fagundes
authors.forename: Patrícia Silva
authors.initials: PS
authors.lastname: Cisalpino
authors.forename: Adailton J
authors.initials: AJ
authors.lastname: Bortoluzzi
authors.forename: Giovanni F
authors.initials: GF
authors.lastname: Caramori
authors.forename: Rafael
authors.initials: R
authors.lastname: de Mattos Piccoli
authors.forename: Hugo T S
authors.initials: HT
authors.lastname: Braibante
authors.forename: Mara E F
authors.initials: ME
authors.lastname: Braibante
authors.forename: Moacir G
authors.initials: MG
authors.lastname: Pizzolatti
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D011804:Quinolines / Q000737:chemistry*; D013055:Spectrophotometry, Infrared
chemical_list: D000935:Antifungal Agents; D000970:Antineoplastic Agents; D047188:Chalcones; D011804:Quinolines