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A series of CAPE derivatives with mono-substituted phenylethanols moiety were synthesized and evaluated by MTT assay on growth of 4 human cancer cell lines (Hela, DU-145, MCF-7 and ECA-109). The substituent effects on the antiproliferative activity were systematically investigated for the first time. It was found that electron-donating and hydrophobic substituents at 2?-position of phenylethanol moiety could significantly enhance CAPE’s antiproliferative activity. 2?-Propoxyl derivative, as a novel caffeic acid ester, exhibited exquisite potency (IC50 = 0.4 ± 0.02 & 0.6 ± 0.03 muM against Hela and DU-145 respectively).
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