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
M. Loriga et al., 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, Il Farmaco, 52(8-9), 1997, pp. 531-537
Thirty quinoxalines bearing a substituted anilino group on position 2,
a carboethoxy or carboxy group on position 3 and a trifluoromethyl gr
oup on position 6 or 7 of the heterocycle were prepared in order to ev
aluate in vitro anticancer activity. Preliminary screening performed a
t NCI showed that most derivatives exhibited a moderate to strong grow
th 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.