Discovery and structural optimization of 4-(4-(benzyloxy) phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists

	Discovery and structural optimization of 4-(4-(benzyloxy) phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists
	Wu Xishan 1; Wang Rui 2; Xing Yanli 2; Xue Xiaoqian 2; Zhang Yan 2; Lu Yongzhi 2; Song Yu 2; Luo Xiaoyu 2; Wu Chun 2; Zhou Yulai 4
刊名	ACTA PHARMACOLOGICA SINICA
	2016
卷号	37 期号:11 页码:1516
关键词	GAMMA-T ORPHAN RECEPTORS CELL-DIFFERENTIATION LIGAND IDENTIFICATION MODULATORS DERIVATIVES PROTEIN INHIBITORS DOCKING nuclear receptor RORc inverse agonist SAR structure-based optimization autoimmune disease
ISSN号	1671-4083
英文摘要	Aim: Retinoic acid receptor-related orphan nuclear receptors (RORs) are orphan nuclear receptors that show constitutive activity in the absence of ligands. Among 3 subtypes of RORs, RORc is a promising therapeutic target for the treatment of Th17-mediated autoimmune diseases. Here, we report novel RORc inverse agonists discovered through structure-based drug design.
资助项目	[National Natural Science Foundation of China] ; ["100 Talents Project" of Chinese Academy of Sciences] ; [Natural Science Foundation of Guangdong Province] ; [Guangzhou Healthcare Collaborative Innovation Programs] ; [Chinese Academy of Sciences Cloud Platform for Stem Cell and Biomedical Research] ; [National Key Basic Research Program of China (973 Program)] ; [Bureau of Science and Information Technology of Guangzhou Municipality] ; [Guangzhou Branch of the Supercomputing Center of Chinese Academy of Sciences]
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/293849]
专题	中国科学院上海药物研究所
作者单位	1.中国科学院上海药物研究所 2.中国科学院 3.中国科学院大学 4.吉林大学
推荐引用方式 GB/T 7714	Wu Xishan,Wang Rui,Xing Yanli,et al. Discovery and structural optimization of 4-(4-(benzyloxy) phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists[J]. ACTA PHARMACOLOGICA SINICA,2016,37(11):1516.
APA	Wu Xishan.,Wang Rui.,Xing Yanli.,Xue Xiaoqian.,Zhang Yan.,...&Xu Yong.(2016).Discovery and structural optimization of 4-(4-(benzyloxy) phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists.ACTA PHARMACOLOGICA SINICA,37(11),1516.
MLA	Wu Xishan,et al."Discovery and structural optimization of 4-(4-(benzyloxy) phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists".ACTA PHARMACOLOGICA SINICA 37.11(2016):1516.