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KMID : 0043320080310080995
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Archives of Pharmacal Research
2008 Volume.31 No. 8 p.995 ~ p.998
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Synthesis and Cytotoxic Activities of 2-Alkyl-2,3-dihydro-1H-2,6,9-triazacyclopenta[b]anthracene-5,10-diones
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Kwak Jae-Hwan
Namgoong Kwon
Jung Jae-Kyung
Cho Jung-Sook
Kim Hwan-Mook
Park Sung-Gyu
Yoo Yeong-Ah
Kwon Joo-Hee
Lee Hee-Soon
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Abstract
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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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KEYWORD
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Cytotoxic activity, Triazacyclopenta[b]anthracene-5, 10-diones
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