Abstract
3-Ethoxycarbonyl-3-methyl-1 N-substrituted-2,3-dihydro-pyridin[2,3- f]indole-2,4,9-trione [ 9(a– d)] and 3-ethoxycarbonyl-3-methyl- N-substrituted-2,3-dihydro-benz[ f]indole-2,4,9-trione [ 10(a– i)] derivatives were synthesized from 7-chloro-6-(1,1-diethoxycarbonyl-ethyl)-5,8-quinolinedione ( 7) and 2-chloro-3-(1,1-diethoxycarbonyl-ethyl)-1,4-naphthoquinone ( 8), respectively, using a variety of alkyl- and arylamines. The cytotoxic activities of the synthesized compounds were evaluated by a Sulforhodamine B (SRB) assay against the following tumor cell lines: A459 (human non-small cell lung), SK-OV-3 (human ovarian), SK-MEL-2 (human melanoma), XF498 (human CNS), and HCT 15 (human colon). Almost all the derivatives mentioned above had a more potent cytotoxic effect against SK-OV-3 than etoposide. In particular, 3-ethoxycarbonyl-3-methyl- N-(4-aminophenyl)-2,3-dihydro-benz[ f]indole-2,4,9-trione ( 10h) exhibited greater activity against all the tumor cell lines, and its cytotoxic effect against SK-OV-3 was especially higher than doxorubicin.
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