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KMID : 0043320120350122093
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Archives of Pharmacal Research
2012 Volume.35 No. 12 p.2093 ~ p.2104
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Synthesis and in vitro antitumor activities of xanthone derivatives containing 1,4-disubstituted-1,2,3-triazole moiety
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Zou Yan
Zhao Qingjie
Hu Honggang
Hu Lina
Yu Shichong
Xu Mingjuan
Wu Qiuye
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Abstract
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To explore the more active antitumor compounds, two series of new xanthones, containing 1,4-disubstituted-1,2,3-triazole moiety were designed and synthesized. Eaton’s Reagent and “click reaction” were used in the synthesis. Most of the title compounds showed good inhibitory activity against the hepatoma carcinoma cell line (Bel-7402) and human cervical carcinoma cell line (HeLa) in vitro. Compounds 10a, 10e, 10f, 11r and 11t had potent activity with IC50 values, ranging from 2.2 ± 0.17 to 7.1 ± 0.27 ∝M, which was equivalent to Doxorubicin.
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KEYWORD
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Xanthone, 1, 2, 3-Triazoles, Click chemistry, Antitumor activity
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