Synthesis, anticancer and cytostatic activity of some 6H-indolo[2,3-b]quinoxalines.
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 C50 of 23 micromol L(-1) against Molt 4/C8 and 38 micromol L(-1) against CEM compared to melphalan 3.2 micromol L(-1) and 2.5 micromol L(-1), respectively. The IC(50) for compound 7i against L1210 was 7.2 micromol L(-1) compared to melphalan 2.1 micromol L(-1).
Karki
Subhas S
SS
Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560010, India. subhasskarki@gmail.com
Hazare
Rahul
R
Kumar
Sujeet
S
Bhadauria
Vivek S
VS
Balzarini
Jan
J
De Clercq
Erik
E
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D054697:Cytostatic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D045563:Indolequinones / Q000138:chemical synthesis / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007939:Leukemia L1210 / Q000139:chemically induced; D008558:Melphalan / Q000494:pharmacology; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy; D013601:T-Lymphocytes / Q000187:drug effects / Q000473:pathology
D000970:Antineoplastic Agents; D054697:Cytostatic Agents; D045563:Indolequinones; D008558:Melphalan