Synthesis and in vitro Evaluation of 7-Dialkylaminomethylbenzo[g]quinoxaline-5,10-diones. -The title compounds (VI) are tested for their cytotoxic activities against four human cancer cell lines. The most active compound (VIc) shows cytotoxic activity comparable to that of doxorubicin against HCT-15 cancer cell lines. -(LEE*, H.; CHO, S.; NAMGOONG, K.; JUNG, J.-K.; CHO, J.; YANG, S.-I.; Bioorg.
A series of 8-alkyl- and 8-aryl-8,9-dihydro-7H-isoindolo[5,6- g]quinoxaline-7,9-diones were synthesized using sultine chemistry as a key step in good yield. These compounds were evaluated for their in vitro cytotoxicity against six human cancer cell lines (HCT15, SK-OV-3, A549, SNB19, MCF7 and MCF7/ADR).
A series of 2-alkyl-2,3-dihydro-1H-2,6,9-triazacyclopenta[b]anthracene-5,10-diones (4a-f) were synthesized and their in vitro cytotoxic activities were evaluated against six human cancer cell lines (HCT15, SK-OV-3, A549, SNB19, MCF7 and MCF7/ADR). A number of compounds including 4c and 4d showed 2-180 times more potent cytotoxic activity than doxorubicin against all human cancer cell lines tested. Furthermore, these compounds retained considerable cytotoxic activity against the doxorubicin-resistant cell line MCF7/ADR, implying their therapeutic potential to treat doxorubicin-resistant tumors.
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