Design, synthesis, and biological evaluation of a new class of MT2-selective agonists
文献类型：期刊论文
| 作者 | Zhang, Xuan1 ; Wang, Zhilong2; Huang, Qingqing1; Luo, Yu1; Xie, Xin2; Lu, Wei1
|
| 刊名 | RSC ADVANCES
 |
| 出版日期 | 2014 |
| 卷号 | 4期号:49页码:25871-25874 |
| ISSN号 | 2046-2069 |
| DOI | 10.1039/c4ra03728f |
| 文献子类 | Article |
| 英文摘要 | A novel class of chiral 2,3-dihydro-1H-indene derivatives were designed and synthesized as melatonergic ligands. Most of the reported MT2-selective ligands behave as antagonists. By contrast, our exploration of 2,3-dihydro-1H-indene showed that the introduction of a lipophilic group at the 2- or 3-position of this scaffold could afford highly selective MT2 agonists. Among all these synthesized molecules, compounds 10b, 12a, 17a, 20a exhibited powerful MT2 agonistic activity (EC50 < 50 nM) as well as excellent MT2 selectivity (more than 2200-fold). |
| WOS关键词 | MELATONIN RECEPTOR AGONISTS ; ANTIPROLIFERATIVE ACTIVITY ; DOUBLE-BLIND ; MT2 ; DERIVATIVES ; ANTAGONISTS ; LIGANDS ; ANALOGS ; CANCER ; SLEEP |
| 资助项目 | State Key Laboratory of Drug Research[SIMM1203KF-10] ; National Natural Science Foundation of China[81172936] ; National Natural Science Foundation of China[21102046] ; Fundamental Research Funds for the Central Universities[00000000] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000338434500050 |
| 出版者 | ROYAL SOC CHEMISTRY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277280]  |
| 专题 | 国家新药筛选中心 中国科学院上海药物研究所 |
| 通讯作者 | Lu, Wei |
| 作者单位 | 1.E China Normal Univ, Inst Drug Discovery & Dev, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai 200062, Peoples R China; 2.Chinese Acad Sci, Natl Ctr Drug Screening, CAS Key Lab Receptor Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Xuan,Wang, Zhilong,Huang, Qingqing,et al. Design, synthesis, and biological evaluation of a new class of MT2-selective agonists[J]. RSC ADVANCES,2014,4(49):25871-25874. |
| APA | Zhang, Xuan,Wang, Zhilong,Huang, Qingqing,Luo, Yu,Xie, Xin,&Lu, Wei.(2014).Design, synthesis, and biological evaluation of a new class of MT2-selective agonists.RSC ADVANCES,4(49),25871-25874. |
| MLA | Zhang, Xuan,et al."Design, synthesis, and biological evaluation of a new class of MT2-selective agonists".RSC ADVANCES 4.49(2014):25871-25874. |
入库方式： OAI收割
来源：上海药物研究所
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