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题名: Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists
作者: 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
发表日期: 2017-01-12
DOI: 10.1021/acs.jmedchem.6b01431
卷: 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
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.
关键词[WOS]: TYROSINE-PHOSPHATASE 1B ;  GPR35 AGONISTS ;  KYNURENIC ACID ;  SELECTIVE AGONISTS ;  IDENTIFICATION ;  POTENT ;  INHIBITORS ;  DESIGN ;  RECRUITMENT ;  METABOLITES
语种: 英语
WOS记录号: WOS:000392035100024
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/151875
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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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

Recommended Citation:
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.
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