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Synthesis of (E)‐5‐Methoxy‐2‐styryl‐4‐pyrones as Potent Growth‐Inhibitory Agents Against Hepatocellular Carcinoma Cells
Authors:Yu‐Hua Chen  Pei‐Jung Lu  Christopher Hulme  Arthur Y Shaw
Institution:1. Department of Chemistry, Tamkang University, New Taipei City, Taiwan;2. Institute of Clinical Medicine, National Cheng Kung University, Tainan, Taiwan;3. Department of Pharmacology and Toxicology, College of Pharmacy, The University of Arizona, Tucson, AZ, USA;4. BIO5 Oro Valley, The University of Arizona, Oro Valley, AZ, USA
Abstract:The present study a series of (E)‐5‐methoxy‐2‐styryl‐4H‐pyran‐4‐ones 6a , 6b , 6c , 6d , 6e , 6f , 6g , 6h , 6i , 6j was synthesized and evaluated for growth inhibitory inhibition against carcinoma cells. The growth inhibition study of eight carcinoma cell lines was examined and demonstrated that SKHep cells exhibit significant structure‐activity relationship in response to the tested compounds. Among them, 6f showed the most potent activity against SKHep, A549, AGS, and H460 cell lines with GI50 values of 0.17, 8.3, 3.6, 8.0 μM, respectively.
Keywords:Arbuzov reaction  Horner‐Emmons reaction  growth‐inhibitory agents  kojic acid  carcinoma cells
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