title: Quinoxaline chemistry. Part 8. 2-[Anilino]-3-[carboxy]-6(7)-substituted quinoxalines as non classical antifolate agents. Synthesis and evaluation of in vitro anticancer, anti-HIV and antifungal activity.
abstract: Thirty quinoxalines bearing a substituted anilino group on position 2, a carboethoxy or carboxy group on position 3 and a trifluoromethyl group on position 6 or 7 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI showed that most derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10(-5) and 10(-4) molar concentrations. Interesting selectivities were also recorded between 10(-8) and 10(-6) M for a few compounds. One single compound exhibited good activity against Candida albicans.
authors.affiliation: Istituto di Chimica Farmaceutica, Università di Sassari.
authors.forename: M
authors.initials: M
authors.lastname: Loriga
authors.forename: P
authors.initials: P
authors.lastname: Moro
authors.forename: P
authors.initials: P
authors.lastname: Sanna
authors.forename: G
authors.initials: G
authors.lastname: Paglietti
authors.forename: S
authors.initials: S
authors.lastname: Zanetti
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002176:Candida albicans; D004354:Drug Screening Assays, Antitumor; D005493:Folic Acid Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D008826:Microbial Sensitivity Tests; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D019380:Anti-HIV Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D005493:Folic Acid Antagonists; D011810:Quinoxalines