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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
刊名JOURNAL OF MEDICINAL CHEMISTRY
2017-01-12
DOI10.1021/acs.jmedchem.6b01431
60期:1页:362-372
收录类别SCI
文章类型Article
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
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.
语种英语
WOS记录号WOS:000392035100024
引用统计
文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/151875
专题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
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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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