Cytotoxic Effects of Pyridino[2, 3-f]indole-4, 9-diones on Human Tumor Cell Lines

Abstract

The cytotoxicities of pyridino[2, 3-f]indole-4, 9-dione derivatives were examined against human lung tumor cell lines (A 549), human ovarian tumor cell lines (SK-OV-3), human melanoma tumor cell lines (SK-MEL-2), human CNS tumor cell lines (XF 498) and numan colon tumor cell lines (HCT 15) in vitro using a Sulforhodamine B assay. 3-Ethoxycarbonyl-1-(2-methoxyethyl)-2-methyl-1H-pyridino[2, 3-f]indole-4, 9-dione (5) showed excellent cytotoxicity against XF 498 and HCT 15. The ED₅₀ values of 5 were 0.006 μg/ml against XF 498 and 0.073 μg/ml against HCT 15, while those of doxorubicin were 0.012 and 0.264 μg/ml, respectively. 1-Benzyl-3-ethoxycarbonyl-2-methyl-1H-pyridino[2, 3-f]indole-4, 9-dione (7) (ED₅₀ value 0.065 μg/ml) was also significanty more cytotoxic against HCT 15 compared with doxorubicin.