Discovery of 2-oxo-1, 2-dihydrobenzo [cd] indole-6-sulfonamide derivatives as new RORγ inhibitors using virtual screening, synthesis and biological evaluation

…, Y Song, J Li, X Luo, M Song, W Yan, H Song…

Index: Zhang, Yan; Xue, Xiaoqian; Jin, Xiangyu; Song, Yu; Li, Jing; Luo, Xiaoyu; Song, Ming; Yan, Weiqun; Song, Hongrui; Xu, Yong European Journal of Medicinal Chemistry, 2014 , vol. 78, p. 431 - 441

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Citation Number: 12

Abstract

Abstract Retinoic acid receptor-related orphan receptor γ (RORγ), a member of the nuclear hormone receptor superfamily, is a promising therapeutic target for treating Th17-mediated autoimmune diseases. We performed structure-based virtual screening targeting the RORγ ligand-binding domain. Among the tested compounds, s4 demonstrated RORγ antagonistic activities with micromolar IC 50 values in both an AlphaScreen assay (20.27 μM) and a ...