Quinoxaline chemistry - Part 12. 3-carboxy-2[phenoxy]-6(7)substituted quinoxalines and N-[4-(6(7) substituted-3-carboxyquinoxalin-2-yl)hydroxy] benzoylglutamates. Synthesis and evaluation of in vitro anticancer activity

Thirty quinoxalines bearing a substituted phenoxy or hydroxybenzoylglutamat e group on position 2, a carboethoxy or carboxy group on position 3 and a t rifluoromethyl group on position 6 or 7 of the heterocycle were prepared in order to evaluate the in vitro anticancer activity. Screening over 21 comp ounds selected at the National Cancer Institute (Bethesda, MD) showed that only few derivatives exhibited a moderate growth inhibition activity on var ious tumor panel cell lines at 10(-4) molar concentration. The acid derivat ives showed no growth inhibition activity. The results obtained in this ser ies 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. (C) 1998 Elsevier Science S.A. All rights reserved.