Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists
文献类型：期刊论文
| 作者 | Shi, Liying1; Wei, Lai1; Wang, Jixia1; Zhang, Xiuli1,3; Wang, Ping1; Zhao, Yaopeng1; Li, Jiaqi1; Hou, Tao1; Qu, Lala1; Liang, Xinmiao1,3 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 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 |
| 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. |
入库方式： OAI收割
来源：大连化学物理研究所
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