Acta Pharmaceutica, Vol. 59 No. 4, 2009.
Izvorni znanstveni članak
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
Sažetak
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 mL1 against Molt 4/C8 and 117 μmol mL1 against CEM compared to melphalan 3.2 μmol mL1 and 2.5 μmol mL1, respectively. The IC50 for compound 7i against L1210 was 7.2 μmol mL1 compared to melphalan 2.1 μmol mL1.
Ključne riječi
indolo[2,3-b]quinoxaline; cytostatic activity; anticancer activity
Hrčak ID:
41024
URI
Datum izdavanja:
1.12.2009.
Posjeta: 2.351 *