Synthesis and in Vitro cytotoxic activities of 2-alkyl-2,3-dihydro-1H-2,6-diazacyclopenta[b]anthracene-5,10-diones |
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| Authors: | Jae-Hwan Kwak Kwon Namgoong Jae-Kyung Jung Sang-Bae Han Jungsook Cho Hwan-Mook Kim Song-Gyu Park Kiho Lee Jong Soon Kang Heesoon Lee |
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| Affiliation: | 1.College of Pharmacy,Chungbuk National University,Cheongju,Korea;2.College of Medicine,Dongguk University,Gyeongju,Korea;3.Korea Research Institute of Bioscience and Biotechnology,Chungbuk,Korea |
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| Abstract: | 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. The most active compound 4c was equipotent with doxorubicin against HCT15 cell line. |
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