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)
  • Published : 2004.06.01

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

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