Abstract
Caffeic acid phenethyl ester (CAPE, 2) and its twenty analogues ( 1, 3– 21) were prepared. These esters were tested by MTT assay on growth of murine colon 26-L5 carcinoma, murine B16-BL6 malonoma, murine Lewis lung carcinoma, human HT-1080 fibrosarcoma, human lung A549 adenocarcinoma, and human cervix HeLa adenocarcinoma cell lines. It was found that CAPE analogues possessed selective antiproliferative activity toward highly liver-metastatic murine colon 26-L5 carcinoma cell line. Among them, 4-phenylbutyl caffeate ( 4), ( Z)-8-phenyl-7-octenyl ( 10a) and ( E)-8-phenyl-7-octenyl ( 10b) caffeate showed the most potent antiproliferative activity (EC 50 value, 0.02 μM). In addition, CAPE ( 2) induced DNA fragmentation at concentrations of 1 to 10 μg/mL towards murine colon 26-L5 carcinoma cells.
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