Synthesis and biological evaluation of retinoid-chalcones as inhibitors of colon cancer cell growth
Published on Wednesday, 10 September 2014
Abstract
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-tetrahydronaphthalen-2-yl)prop-1-enyl)benzonitrile 8 showed submicromolar inhibitory activity with an IC(50) of 0.66 μM.
Supplementary Data
See also All-Trans-Retinoic Acid (ATRA - analogues and/or derivatives).