Antitumorigenic Activities of Chalcones. I. Inhibitory Effects of Chalcone Derivatives on 32Pi-Incorporation Into Phospholipids of Hela Cells Promoted by 12-O-Tetradecanoyl-Phorbol 13-Acetate(TPA).

Abstract

More than forty chalcone derivatives were synthesized to examine their structure-activity relationship against tumorigenesis. As a primary screening test, the inhibitory activities of the chalcones for the 32Pi-incorporation into phospholipids of HeLa cells enhanced by 12-O-tetradecanoyl-phorbol 13-acetate (TPA) were examined. 3-Hydroxy-chalcone derivatives possessing methyl group in 3´-, 4´-, or 2´-position and isoliquiritigenin homologs showed potent inhibitory activities in the phosphorylation test, which suggests their antitumorigenic effects. © 1995, The Pharmaceutical Society of Japan. All rights reserved.