Quinoxaline chemistry. Part 5. 2- (R) -benzylaminoquinoxalines as nonclassical antifolate agents. Synthesis and evaluation of in vitro anticancer activity
Loriga, M.; Fiore, M.; Sanna, P.; Paglietti, G.
Farmaco 51(8-9): 559-568
1996
ISSN/ISBN: 0014-827X PMID: 8930109 Document Number: 459064
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.