Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists

	Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists
	Shi, Liying 1; Wei, Lai 1; Wang, Jixia 1; Zhang, Xiuli 1,3; Wang, Ping 1; Zhao, Yaopeng 1; Li, Jiaqi 1; Hou, Tao 1; Qu, Lala 1; Liang, Xinmiao 1,3
刊名	JOURNAL OF MEDICINAL CHEMISTRY
	2017-01-12
卷号	60 期号:1 页码:362-372
英文摘要	A family of 2H-chromen-2-one derivatives were identified as G protein-coupled receptor-35 (GPR35) agonists using dynamic mass redistribution assays in HT-29 cells. The compounds with 1H-tetrazol-5-y1 in 3-substituted position displayed higher potency than the corresponding carboxyl analogs, and the hydroxyl group in the 7-position also played an important role in GPR35 agonistic activity. 6-Bromo-7-hydroxy-8-nitro-3-(1H-tetrazol-5-71)-2H-chromen-2-one (50) was found to be the most potent GPR35 agonist with an EC50 of 5.8 nM. Calculating the physicochemical properties of compounds with moderate to high potency suggested that compounds 30, 50, and 51 showed good druggability. This study provides a novel series of GPR35 agonists, and compound 50 may be a powerful tool to study GPR35.
WOS标题词	Science & Technology ; Life Sciences & Biomedicine
类目[WOS]	Chemistry, Medicinal
研究领域[WOS]	Pharmacology & Pharmacy
关键词[WOS]	TYROSINE-PHOSPHATASE 1B ; GPR35 AGONISTS ; KYNURENIC ACID ; SELECTIVE AGONISTS ; IDENTIFICATION ; POTENT ; INHIBITORS ; DESIGN ; RECRUITMENT ; METABOLITES
收录类别	SCI
语种	英语
WOS记录号	WOS:000392035100024
内容类型	期刊论文
源URL	[http://cas-ir.dicp.ac.cn/handle/321008/151875]
专题	大连化学物理研究所_中国科学院大连化学物理研究所
作者单位	1.Chinese Acad Sci, Dalian Inst Chem Phys, Key Lab Separat Sci Analyt Chem, Dalian 116023, Peoples R China 2.Biochem Technol Sci & Technol Div, Corning, NY 14831 USA 3.Nantong Univ, Coinnovat Ctr Neuroregenerat, Nantong 226019, Peoples R China
推荐引用方式 GB/T 7714	Shi, Liying,Wei, Lai,Wang, Jixia,et al. Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists[J]. JOURNAL OF MEDICINAL CHEMISTRY,2017,60(1):362-372.
APA	Shi, Liying.,Wei, Lai.,Wang, Jixia.,Zhang, Xiuli.,Wang, Ping.,...&Fang, Ye.(2017).Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists.JOURNAL OF MEDICINAL CHEMISTRY,60(1),362-372.
MLA	Shi, Liying,et al."Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists".JOURNAL OF MEDICINAL CHEMISTRY 60.1(2017):362-372.