Synthesis and biological evaluation of retinoid-chalcones as inhibitors of colon cancer cell growth |
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| Authors: | Mizuno Cassia S Paul Shiby Suh Nanjoo Rimando Agnes M |
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| Affiliation: | US Department of Agriculture, Agricultural Research Service, Natural Products Utilization Research Unit, University, MS 38677, USA. cmizuno@olemiss.edu |
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| 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. |
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