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KMID : 0043320100330050663
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Archives of Pharmacal Research
2010 Volume.33 No. 5 p.663 ~ p.667
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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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Lee Hee-Soon
Kwak Jae-Hwan
Kwon Nam-goong
Jung Jae-Kyung
Han Sang-Bae
Cho Jung-Sook
Kim Hwan-Mook
Park Song-Gyu
Lee Ki-Ho
Kang Jong-Soon
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Abstract
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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 doxorubicinresistant 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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KEYWORD
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Cytotoxic activity, Diazacyclopenta[b]anthracene-5, 10-diones
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