Mechanism of toxicity of esters of caffeic and dihydrocaffeic acids

Ten esters each of caffeic acid and dihydrocaffeic acid have recently been synthesized. Cytotoxicity evaluations of these esters versus L1210 leukemia and MCF-7 breast cancer cells in culture have led to the delineation of su bstantially different QSAR for each series. The L1210 QSAR for dihydrocaffe ic acid esters resembles the QSAR obtained for simple phenols and estrogeni c phenols. However, the QSAR pertaining to the caffeic acid esters differs considerably from its sister QSAR. This difference may be attributed to the presence of the olefinic linkage in the side chain. The octyl ester of caf feic acid is nearly ten times as toxic to the leukemia cells than the widel y studied phenethyl ester, CAFE. (C) 2000 Elsevier Science Ltd. All rights reserved.