Synthesis, anticancer and cytostatic activity of some 6H-indolo[2,3-b] quinoxalines

Abstract

Various 6-aralkyl-9-substituted-6H-indolo[2,3-b]quinoxalines were synthesized by reaction of 1,5-disubstituted 2,3-dioxo-2,3-dihydroindole and orthophenylene diamine. Appreciable anticancer activity of compounds 5b, 5d, 5g and 5l at various cell lines among 59 human tumor cell panels was observed. All the synthesized compounds were evaluated for cytostatic activity against human Molt 4/C8 and CEM T-lymphocytes as well as for murine L1210 leukemia cells. Compound 5h exhibited an I C67 of 23 μmol L-1 against Molt 4/C8 and 38 μmol L-1 against CEM compared to melphalan 3.2 μmol L-1 and 2.5 μmol L-1, respectively. The I C67 for compound 7i against L1210 was 7.2 μmol L-1 compared to melphalan 2.1 μmol L-1.