Riferimento:
Bioorg Med Chem Lett. 2010 Dec 15;20(24):7385-7.
Autori:
Mizuno CS, Paul S, Suh N, Rimando AM.
Fonte:
Bioorg Med Chem Lett. 2010 Dec 15;20(24):7385-7.
Anno:
2010
Azione:
Ibridi retinoidi calconoidi (classe flavonoidi) sono stati testati contro la linea cellulare di cancro del colon HT-29 mostrando un'attività inibitoria.
Target:
Retinoidi-calconoidi/cancro del colon.
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.
Sostanze: