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  • Title: Quinoxaline chemistry. Part 7. 2-[aminobenzoates]- and 2-[aminobenzoylglutamate]-quinoxalines as classical antifolate agents. Synthesis and evaluation of in vitro anticancer, anti-HIV and antifungal activity.
    Author: Loriga M, Piras S, Sanna P, Paglietti G.
    Journal: Farmaco; 1997 Mar; 52(3):157-66. PubMed ID: 9212450.
    Abstract:
    Thirty-three quinoxalines bearing an aminobenzoyl or aminobenzoylglutamate group on position 2 and various substituents on position 3,6,7 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI 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(-6) M. Among the series examined one compound (29) which was the most active also exhibited both in vitro anti-HIV protection and antifungal activity while in other two (31, 37) the antifungal activity was prevailing.
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