Synthesis and in Vitro cytotoxic activities of 2-alkyl-2,3-dihydro-1H-2,6-diazacyclopenta[b]anthracene-5,10-diones.

A series of 2-alkyl-2,3-dihydro-1H-2,6-diazacyclopenta[b]anthracene-5,10-diones (4a-f) was synthesized and their in vitro cytotoxic activities were evaluated against six human cancer cell lines (HCT15, SK-OV-3, SNB19, A549, MCF7 and MCF7/ADR). They all appeared to be less potent than doxorubicin against all doxorubicin sensitive human cancer cell lines tested. However, these compounds retained considerable cytotoxic activity against the doxorubicin-resistant cell line MCF7/ADR, implying their therapeutic potential to treat doxorubicin-resistant tumors.

Synthesis and cytotoxic activities of 2-alkyl-2,3-dihydro-1H-2,6,9-triazacyclopenta[b]anthracene-5,10-diones.

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.

Synthesis and cytotoxic activities of 8-alkyl or 8-aryl-8,9-dihydro-7H-isoindolo[5,6-g]quinoxaline-7,9-diones.

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).

Synthesis and in vitro evaluation of 7-dialkylaminomethylbenzo[g]quinoxaline-5,10-diones.

A series of benzo[g]quinoxaline-5,10-dione derivatives carrying a 7-dialkylaminomethyl substituent was synthesized and their in vitro cytotoxic activities were evaluated against four human cancer cell lines (HCT-15, SK-OV-3, MD-MB-468 and T-47D). The most active compound 9d showed cytotoxic activity comparable to that of doxorubicin against HCT-15 cancer cell line.