Acta Pharm. 59 (2009) 431-440

full paper

Original research paper

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

SUBHAS S. KARKI, RAHUL HAZARE, SUJEET KUMAR, VIVEK S. BHADAURIA, JAN BALZARINI and ERIK De CLERCQ

subhasskarki@gmail.com

¹Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560010, India

²Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium

Accepted October 22, 2009

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 with 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 IC₅₀ of 71 μmol mL^-1 against Molt 4/C8 and 117 μmol mL^-1 against CEM compared to melphalan 3.2 μmol mL^-1 and 2.5 μmol mL^-1, respectively. The IC₅₀ for compound 7i against L1210 was 7.2 μmol mL^-1 compared to melphalan 2.1 μmol mL^-1.

Keywords: indolo[2,3-b]quinoxaline, cytostatic activity, anticancer activity