<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml">Various 6-aralkyl-9-substituted-6<italic>H</italic>-indolo[2,3-<italic>b</italic>]quinoxalines were synthesized by
reaction of 1,5-disubstituted 2,3-dioxo-2,3-dihydroindole with orthophenylene diamine.
Appreciable anticancer activity of compounds <bold>5b</bold>, <bold>5d</bold>, <bold>5g</bold> and <bold>5l</bold> 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 <bold>5h</bold> exhibited an <italic>IC</italic>50
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 <italic>IC</italic>50 for
compound <bold>7i</bold> against L1210 was 7.2 µmol mL-1

compared to melphalan 2.1 µmol
mL-1.</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.

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

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

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

Acta Pharmaceutica

Synthesis, anticancer and cytostatic activity of some 6-indolo[2,3-]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 with orthophenylene...

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

Publié en ligne: 16 nov. 2009

Pages: 431 - 440

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

Mots clés
indolo[2,3-]kinoksalin, citostatsko djelovanje, antitumorsko djelovanje

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