Original scientific paper

https://doi.org/10.2478/v10007-009-0040-9

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

SUBHAS S. KARKI ; Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560 010, India
RAHUL HAZARE ; Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560 010, India
SUJEET KUMAR ; Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560 010, India
VIVEK S. BHADAURIA ; Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560 010, India
JAN BALZARINI ; Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven Belgium
ERIK De CLERCQ ; Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven Belgium

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 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

Hrčak ID:

41024

URI

https://hrcak.srce.hr/41024

Publication date:

1.12.2009.

Article data in other languages: croatian

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