Study On Design And Synthesis Of Flavonoid Analogues And Small Molecule Inhibitors Of Fatty Acid Binding Protein And Biological Activities

In this paper, analogues based on natural compound Flavonoid have beensynthesized to discover new antitumor candidate agents. The research of smallmolecule inhibitors of Fatty Acid Binding Protein design, synthesis and biologicalactivity made full use of traditional medicinal chemistry design theory and computervirtual screening method to expect better active compounds.1. Design and Synthesis of small molecule inhibitors of EGFRFlavonoids have a variety of anti-tumor mechanism. As a typical flavonoidderivatives, quercetin can significantly inhibit cancer-promoting agent, inhibiting thegrowth of malignant cells in vitro, inhibition of Ehrlich ascites cancer cells DNA,RNA and protein synthesis. This paper designed series of derivatives based on thestructural of Flavonoid to get better anti-cancer active compounds.2. Design, Synthesis and Biological activity of small molecule inhibitors of Fatty AcidBinding Protein4FABP4is one of the most famous in fatty acid binding protein family. Fatty acidbinding protein (FABP4) inhibitor for the treatment of obesity, diabetes,arteriosclerosis and fat have caused widespread concern.FABP4expression in fat cells, is one of important proteins of the adipocytedifferentiation and upregulation. As the transporter of the fatty acid protein, FABP4affect the metabolism and signal transduction of fatty acids. FABP4affects the lipidmetabolism-related gene expression and closely related to the formation ofatherosclerotic plaques. As a potential target for the treatment of type2 diabetes,FABP4inhibitors can improve insulin sensitivity, inhibit development ofatherosclerosis.Based on the results of the laboratory has got, we have Designed and Synthesisedthree series of compounds to get compounds with better inhibitory activity.