Synthesis and biological evaluation of retinoid-chalcones as inhibitors of colon cancer cell growth

[摘要] Based on the observed anticancer activity of chalcones and retinoids, a novel class of retinoid-chalcone hybrids was designed and synthesized. As part of our ongoing studies to discover natural product based anticancer compounds, the retinoid-chalcone hybrids were tested against the colon cancer cell line HT-29. Retinoid like moiety was introduced through Friedel-Crafts alkylation of toluene. Among the synthesized compounds, the cyano derivative (E)-3-(3-oxo-3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetra-hydronaphthalen-2-yl) prop-1-enyl) benzonitrile 8 showed submicromolar inhibitory activity with an IC50 of 0.66 mu M. Published by Elsevier Ltd.

[发布日期] 2010-12-15

[关键词] Chalcones;Retinoids;HT-29 cells;Colon cancer