title: Quinoxaline chemistry. Part 5. 2-(R)-benzylaminoquinoxalines as nonclassical antifolate agents. Synthesis and evaluation of in vitro anticancer activity.
abstract: Thirty-one quinoxalines bearing a substituted benzylamino group on position 2 and various substituents on position 3,6,7 and 8 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI on twenty-two compounds 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(-5) M.
authors.affiliation: Istituto di Chimica Farmaceutica, Università di Sassari.
authors.forename: M
authors.initials: M
authors.lastname: Loriga
authors.forename: M
authors.initials: M
authors.lastname: Fiore
authors.forename: P
authors.initials: P
authors.lastname: Sanna
authors.forename: G
authors.initials: G
authors.lastname: Paglietti
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005493:Folic Acid Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D005493:Folic Acid Antagonists; D011810:Quinoxalines