DICP OpenIR
Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists
Wei, Lai1; Wang, Jixia1; Zhang, Xiuli1,3; Wang, Ping1; Zhao, Yaopeng1; Li, Jiaqi1; Hou, Tao1; Qu, Lala1; Shi, Liying1; Liang, Xinmiao1,3; Fang, Ye2
Source PublicationJOURNAL OF MEDICINAL CHEMISTRY
2017-01-12
DOI10.1021/acs.jmedchem.6b01431
Volume60Issue:1Pages:362-372
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
WOS SubjectChemistry, Medicinal
WOS Research AreaPharmacology & Pharmacy
WOS KeywordTYROSINE-PHOSPHATASE 1B ; GPR35 AGONISTS ; KYNURENIC ACID ; SELECTIVE AGONISTS ; IDENTIFICATION ; POTENT ; INHIBITORS ; DESIGN ; RECRUITMENT ; METABOLITES
AbstractA 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 IDWOS:000392035100024
Citation statistics
Cited Times:5[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/151875
Collection中国科学院大连化学物理研究所
Affiliation1.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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