Author/Authors :
Chika Nakamura، نويسنده , , Nobuhide Kawasaki، نويسنده , , Hideki Miyataka، نويسنده , , Ezhuthachan Jayachandran، نويسنده , , In Ho Kim، نويسنده , , Kenneth L. Kirk، نويسنده , , Takeo Taguchi، نويسنده , , Yoshio Takeuchi، نويسنده , , Hitoshi Hori، نويسنده , , Toshio Satoh، نويسنده ,
Abstract :
We have designed and synthesized new 5-lipoxygenase inhibitors, fluorinated 3,4-dihydroxychalcones, and evaluated their biological activities with respect to antiperoxidation activity and in vitro antitumor activities. All fluorinated chalcones tested showed 5-lipoxygenase inhibition on rat basophilic leukemia-1 (RBL-1) cells and inhibitory action on Fe3+-ADP induced NADPH-dependent lipid peroxidation in rat liver microsomes. The potencies were comparable or better to that of the lead 3,4-dihydroxychalcone. 6-Fluoro-3,4-dihydroxy-2′,4′-dimethoxy chalcone (7) was the most effective compound in the in vitro assay using a human cancer cell line panel (HCC panel) consisting of 39 systems.
