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 synt...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.展开更多
A series of new aurone derivatives was prepared by means of a practical route and their anti-vascular smooth muscle cells（VSMC） vegetation activities were evaluated by the 3-（4,5-dimethylthlazol-2-yl）-2,5- dipheny...A series of new aurone derivatives was prepared by means of a practical route and their anti-vascular smooth muscle cells（VSMC） vegetation activities were evaluated by the 3-（4,5-dimethylthlazol-2-yl）-2,5- diphenyltetrazolium bromide（MTT） method with tetrandrine as a positive contrast drug. The structures of the com- pounds were confirmed by 1H NMR, 13C NMR and electrospray ionization mass spectrometry（ESI-MS）. Several new compounds exhibited promising activity against VSMC proliferation and the preliminary structure-activity relation- ships（SAR） were discussed in order to investigate the essential structures required for their bioactivities.展开更多
基金Supported by the National High-Tech Research and Development Program of China(No.2006AA09Z446)the Fund of State Key Laboratory of Natural and Biomimetic Drags+7 种基金 Peking UniversityChina(No.20080210)the Shanxi Provincial Foundation for Overseas Returned China(No.2009021005)the Program for the Top Young and Middle-aged Innovative Talents of Higher Learning Institutions of Shanxi Province China(No.20091041-1)the Innovative Program of Shanxi Medical University China (No.38)
文摘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.
基金Supported by the National Natural Science Foundation of China(No.81172938)the Program for the Top Science and Technology Innovation Teams of Higher Learning Institutions of Shanxi Province,China+1 种基金the Shanxi Foundation for Overseas Returned,China(No.2008-51)the Program for the Top Young and Middle-aged Innovative Talents of Higher Learning Institutions of Shanxi Province,China
文摘A series of new aurone derivatives was prepared by means of a practical route and their anti-vascular smooth muscle cells（VSMC） vegetation activities were evaluated by the 3-（4,5-dimethylthlazol-2-yl）-2,5- diphenyltetrazolium bromide（MTT） method with tetrandrine as a positive contrast drug. The structures of the com- pounds were confirmed by 1H NMR, 13C NMR and electrospray ionization mass spectrometry（ESI-MS）. Several new compounds exhibited promising activity against VSMC proliferation and the preliminary structure-activity relation- ships（SAR） were discussed in order to investigate the essential structures required for their bioactivities.
