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

• Published in: Farmaco (Società chimica italiana : 1989) Vol. 52; no. 8-9; pp. 531 - 537
• Main Authors: Loriga, M, Moro, P, Sanna, P, Paglietti, G, Zanetti, S
• Format: Journal Article
• Language: English
• Published: LAUSANNE Elsevier 01.08.1997
• Subjects: Anti-HIV Agents - chemical synthesis; Anti-HIV Agents - pharmacology; Antifungal Agents - chemical synthesis; Antifungal Agents - pharmacology; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - pharmacology; Candida albicans; Drug Screening Assays, Antitumor; Folic Acid Antagonists - chemical synthesis; Folic Acid Antagonists - pharmacology; Humans; Life Sciences & Biomedicine; Microbial Sensitivity Tests; Pharmacology & Pharmacy; Quinoxalines - chemical synthesis; Quinoxalines - pharmacology; Science & Technology; STRUCTURE ELUCIDATION
• ISSN: 0014-827X; 1879-0569

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.