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Synthesis and Cytotoxicity of 2,5-Dihydroxychalcones and Related Compounds  

Nam, Nguyen-Hai (College of Pharmacy, Chungnam National University)
Hong, Dong-Ho (College of Pharmacy, Chungnam National University)
You, Young-Jae (College of Pharmacy, Chungnam National University)
Kim, Yong (College of Pharmacy, Chungnam National University)
Bang, Seong-Cheol (College of Pharmacy, Chungnam National University)
Kim, Hwan-Mook (Korea Research Institute of Bio-science and Biotechnology)
Ahn, Byung-Zun (College of Pharmacy, Chungnam National University)
Publication Information
Archives of Pharmacal Research / v.27, no.6, 2004 , pp. 581-588 More about this Journal
Abstract
A series of 2, 5-dihydroxychalcones and related compounds were synthesized, and their cyto-toxicities against tumor cell lines and human umbilical venous endothelial cells (HUVEC） eval-uated. It was found that chalcones, with electron-withdrawing substituents on an A ring, exhibited significant cytotoxicities. Among the synthesized compounds, 2'-chlbro-2, 5-dihydrox-ychalcone (9） was most potent, with an $IC_{50}$ value as low as $0.31{\;}{\mu\textrm{g}}/mL$. This compound also exhibited a significant cytotoxic selectivity toward HUVEC.
Keywords
Chalcone; Cytotoxicity; Structure-activity relationship;
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