Quinoxaline chemistry. Part 5. 2-(R)-benzylaminoquinoxalines as nonclassical antifolate agents. Synthesis and evaluation of in vitro anticancer activity.
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.
Loriga
M
M
Istituto di Chimica Farmaceutica, Università di Sassari.
Fiore
M
M
Sanna
P
P
Paglietti
G
G
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
D000970:Antineoplastic Agents; D005493:Folic Acid Antagonists; D011810:Quinoxalines