The hit-to-lead optimization of 1,2,3,4,4a,9a-hexahydro-1H...

The hit-to-lead optimization of 1,2,3,4,4a,9a-hexahydro-1H-xanthenes as glucocorticoid receptor antagonists Yan-Hui Zhu Meng Zhang Qun-Yi Li Qing Liu Jie Zhang Yun-Yun Yuan Fa-Jun Nan Ming-Wei Wang 【摘要】: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.
《Chinese Chemical Letters》 2014年05期 收藏 | 投稿 | 手机打开 The hit-to-lead optimization of 1,2,3,4,4a,9a-hexahydro-1H-xanthenes as ...Glucocorticoid receptor Antagonist a a-Hexahydroxanthene Structure–activity relationship Lead optimizationGlucocorticoid receptor Antagonist a a-Hexahydroxanthene Structure–activity relationship Lead optimizationThe hit

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