3-(3,4,5-Trimethoxyphenyl)-1-oxo-2-propene: A novel pharmacophore displaying potent multidrug resistance reversal and selective cytotoxicity

This study revealed that various alicyclic and acyclic compounds containing the 3-(3,4,5-trimethoxyphenyl)-2-propenoyl group displayed potent MDR reversal properties. In particular, a concentration of 4 μg/ml of 2,5-bis(3,4,5-trimethoxyphenylmethylene)cyclopentanone was 31 times more potent than verapamil as a MDR revertant. In general, they were selectively toxic to malignant rather than normal cells. Two representative compounds induced apoptosis in human HL-60 cells and markedly activated caspase-3.

The mounting of the 3-(3,4,5-trimethoxyphenyl)-1-oxo-2-propenyl group onto different molecular scaffolds resulted in compounds displaying potent MDR-reversal properties and the ability to display selective cytotoxicity for malignant cells.Figure optionsDownload as PowerPoint slide