QUINOXALINE CHEMISTRY .7. 2-[AMINOBENZOATES]-QUINOXALINES AND 2-[AMINOBENZOYLGLUTAMATE]-QUINOXALINES AS CLASSICAL ANTIFOLATE AGENTS - SYNTHESIS AND EVALUATION OF IN-VITRO ANTICANCER, ANTI-HIV AND ANTIFUNGAL ACTIVITY

Thirty-three quinoxalines bearing an aminobenzoyl or aminobenzoylgluta mmate group on position 2 and various substituents on position 3,6,7 o f the heterocycle were prepared in order to evaluate in vitro anticanc er activity. Preliminary screening performed at NCI showed that most d erivatives exhibited a moderate to strong growth inhibition activity o n various tumor panel cell lines between 10(-5) and 10(-4) Molar conce ntrations. Interesting selectivities were also recorded between 10(-8) and 10(-6) M. Among the series examined one compound (29) which was t he most active also exhibited both in vitro anti-HIV protection and an tifungal activity while in other two (31, 37) the antifungal activity was prevailing.