Vitale, Gabriella and Corona, Paola and Loriga, Mario and Paglietti, Giuseppe (1998) Quinoxaline chemistry: Part 12: 3-carboxy-2[phenoxy]-6(7)substituted quinoxalines and N-[4-(6(7) substituted-3-carboxyquinoxalin-2-yl)hydroxybenzoylglutamates: synthesis and evaluation of in vitro anticancer activity. Il Farmaco, Vol. 53 (8-9), p. 594-601. ISSN 0014-827X. Article.
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Thirty quinoxalines bearing a substituted phenoxy or hydroxybenzoylglutamate group on position 2, a carboethoxy or carboxy group on position 3 and a trifluoromethyl group on position 6 or 7 of the heterocycle were prepared in order to evaluate the in vitro anticancer activity. Screening over 21 compounds selected at the National Cancer Institute (Bethesda, MD) showed that only few derivatives exhibited a moderate growth inhibition activity on various tumor panel cell lines at 10−4 molar concentration. The acid derivatives showed no growth inhibition activity. The results obtained in this series seem to indicate that in general carboxy or carboethoxy groups close to O-link with phenyl or benzoyl glutamates on position 2 are detrimental for anticancer activity.
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