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).
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.
Iwata
S
S
Research Laboratory, Minophagen Pharmaceutical Co., Kanagawa, Japan.
Nishino
T
T
Nagata
N
N
Satomi
Y
Y
Nishino
H
H
Shibata
S
S
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002599:Chalcone / Q000031:analogs & derivatives* / Q000494:pharmacology*; D047188:Chalcones; D002642:Chick Embryo; D005347:Fibroblasts / Q000187:drug effects; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D010743:Phospholipids / Q000378:metabolism*; D010761:Phosphorus Radioisotopes; D013755:Tetradecanoylphorbol Acetate / Q000037:antagonists & inhibitors
D000970:Antineoplastic Agents; D047188:Chalcones; D010743:Phospholipids; D010761:Phosphorus Radioisotopes; D002599:Chalcone; C040920:isoliquiritigenin; D013755:Tetradecanoylphorbol Acetate