1.
Bioorg Med Chem
; 21(2): 388-94, 2013 Jan 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-23245570
RESUMO
A type of novel α,ß-unsaturated cyclohexanone analogous, which designed based on the curcumin core structure, have been discovered as potential EGFR inhibitors. These compounds exhibit potent antiproliferative activity in two human tumor cell lines (Hep G2 and B16-F10). Among them, compounds I(3) and I(12) displayed the most potent EGFR inhibitory activity (IC(50) = 0.43 µM and 1.54 µM, respectively). Molecular docking of I(12) into EGFR TK active site was also performed. This inhibitor nicely fitting the active site might well explain its excellent inhibitory activity.