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

doi:10.1021/acs.jmedchem.6b01431

DICP OpenIR

	Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists
	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; Shi, Liying 1; Liang, Xinmiao 1,3; Fang, Ye 2
Source Publication	JOURNAL OF MEDICINAL CHEMISTRY
	2017-01-12
DOI	10.1021/acs.jmedchem.6b01431
Volume	60 Issue:1 Pages:362-372
Indexed By	SCI
Subtype	Article
WOS Headings	Science & Technology ; Life Sciences & Biomedicine
WOS Subject	Chemistry, Medicinal
WOS Research Area	Pharmacology & Pharmacy
WOS Keyword	TYROSINE-PHOSPHATASE 1B ; GPR35 AGONISTS ; KYNURENIC ACID ; SELECTIVE AGONISTS ; IDENTIFICATION ; POTENT ; INHIBITORS ; DESIGN ; RECRUITMENT ; METABOLITES
Abstract	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.
Language	英语
WOS ID	WOS:000392035100024
Citation statistics
Document Type	期刊论文
Identifier	http://cas-ir.dicp.ac.cn/handle/321008/151875
Collection	中国科学院大连化学物理研究所
Affiliation	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
Recommended Citation GB/T 7714	Wei, Lai,Wang, Jixia,Zhang, Xiuli,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	Wei, Lai.,Wang, Jixia.,Zhang, Xiuli.,Wang, Ping.,Zhao, Yaopeng.,...&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	Wei, Lai,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.

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