Synthesis of New Flavanone Derivatives of Farrerol and Preliminary SAR Studies on Anti-VSMCs Vegetat

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A series of new flavanone derivatives of farrerol was designed and synthesized as a potent inhibitor of vascular smooth muscle cells(VSMCs) vegetation according to a convenient method. The structures of all the synthesized compounds were confirmed by 1H NMR, 13C NMR and EIHR-MS. The biological activities of these compounds against VSMCs in vitro were evaluated. The assay results indicate that two compounds, 5,7-dihydroxy-6,8-dimethyl- 2-(2-nitrophenyl)chroman-4-one(7f) and 2,3-dibromo-4,5-dihydroxydiphenylmethanone(7j) exhibited high activity against VSMCs in vitro with IC50 values of 9.9 and 6.7 μmol/L, respectively, and the preliminary structure-activity relationship(SAR) was described. A series of new flavanone derivatives of farrerol was designed and synthesized as a potent inhibitor of vascular smooth muscle cells (VSMCs) vegetation according to a convenient method. The structures of all the example compounds were confirmed by 1H NMR, 13C NMR and EIHR-MS . The biological activities of these compounds against VSMCs in vitro were evaluated. The assay results indicate that two compounds, 5,7- dihydroxy-6,8-dimethyl- 2- (2-nitrophenyl) chroman-4-one 2,3-dibromo-4,5-dihydroxydiphenylmethanone (7j) exhibited high activity against VSMCs in vitro with IC50 values ​​of 9.9 and 6.7 μmol / L, respectively, and the preliminary structure-activity relationship (SAR) was described.
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