Subject Code:C05With the support by the National Natural Science Foundation of China,a team of scientists let by Profs.Wu Beili(吴蓓丽),Wang Mingwei and Jiang Hualiang from Shanghai Institute of Materia Medica,Chinese...Subject Code:C05With the support by the National Natural Science Foundation of China,a team of scientists let by Profs.Wu Beili(吴蓓丽),Wang Mingwei and Jiang Hualiang from Shanghai Institute of Materia Medica,Chinese Academy of Sciences has determined the high-resolution atomic structure of a full-length class B展开更多
The structure–activity relationship（SAR） study of a 1 2 3 4 4a 9a-hexahydro-1H-xanthene series of selective,human glucocorticoid receptor a（hGRa） antagonists is reported.Compounds were screened using hydroxyapati...The structure–activity relationship（SAR） study of a 1 2 3 4 4a 9a-hexahydro-1H-xanthene series of selective,human glucocorticoid receptor a（hGRa） antagonists is reported.Compounds were screened using hydroxyapatite-based GR binding and MMTV-Luc co-transfection reporter gene assays.Four different regions of the scaffold were modified to assess the effects on hGRa antagonism and related potency.Compound 8d exhibits an 8-fold better bioactivity than the original hit 1a,as well as an improved chemical stability,which make it a promising lead for the subsequent optimization.展开更多
文摘Subject Code:C05With the support by the National Natural Science Foundation of China,a team of scientists let by Profs.Wu Beili(吴蓓丽),Wang Mingwei and Jiang Hualiang from Shanghai Institute of Materia Medica,Chinese Academy of Sciences has determined the high-resolution atomic structure of a full-length class B
基金supported in part by grants from the Ministry of Health of China (Nos. 2012ZX09304-011, 2013ZX09401003-005, 2013ZX09507001 and 2013ZX09507002)Shanghai Science and Technology Development Fund (No. 13DZ2290300)Thousand Talents Program in China
文摘The structure–activity relationship（SAR） study of a 1 2 3 4 4a 9a-hexahydro-1H-xanthene series of selective,human glucocorticoid receptor a（hGRa） antagonists is reported.Compounds were screened using hydroxyapatite-based GR binding and MMTV-Luc co-transfection reporter gene assays.Four different regions of the scaffold were modified to assess the effects on hGRa antagonism and related potency.Compound 8d exhibits an 8-fold better bioactivity than the original hit 1a,as well as an improved chemical stability,which make it a promising lead for the subsequent optimization.
