Preparation Of Coffee Ester Derivatives And Their Biological Activity

Cancer and AIDS are the most dangerous diseases that endanger human beings. It is one of the main fields of the new drug research to seek for a new antitumor drug of high effectivity and low toxicity. In this dissertation, we disclosed our research results on the synthesis of caffeic acid ester derivatives as a kind of natural drugs and their biological activities. There are three achievements provided such as:1 We prepared a series of aldehyde from vanillin, and then, these aldehydes were reacted with alcohols to form caffeic acid esters by using a convenient one-pot synthetic method. As a result, 18 compounds including 13 new compounds were synthesized by this method.2 The synthesized compounds were characterized by IR.. ~1H NMR MS and EA. The coupling constants (J=15.9 or 16.0Hz) of a-H and 6-H indicate that caffeic acid esters prepared by this methods are trans (E) form in accordance with the configuration of the natural esters.3 The anti-tumor tests in vitro of the synthesized compounds were carried on HL-60 human leucocythemia cells and anti-HIV integrase cells, and some compounds indicated good anti-HIV integrase activity. 5-nitryl caffeic acid esters displayed stronger activity than the lead compound— caffeic acid phenylethyl ester (CAPE).It shows the evidence that this kind of caffeic acid esters displayed a good anti-HIV integrase activity...