Function-Oriented Synthesis of Marine Phidianidine Derivatives as Potential PTP1B Inhibitors with Specific Selectivity
文献类型：期刊论文
| 作者 | Liu, Jin1,2; Chen, Yu1; Li, Jing-Ya1 ; Luo, Cheng1,3; Li, Jia1,3; Chen, Kai-Xian1,3; Li, Xu-Wen1,3; Guo, Yue-Wei1,3
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| 刊名 | MARINE DRUGS
 |
| 出版日期 | 2018-03 |
| 卷号 | 16期号:3 |
| 关键词 | phidianidine marine natural products PTP1B inhibitor specific selectivity docking analysis Function Oriented Synthesis structure-activity relationship |
| ISSN号 | 1660-3397 |
| DOI | 10.3390/md16030097 |
| 文献子类 | Article |
| 英文摘要 | Phidianidines A and B are two novel marine indole alkaloids bearing an uncommon 1,2,4-oxadiazole ring and exhibiting various biological activities. Our previous research showed that the synthesized phidianidine analogs had the potential to inhibit the activity of protein tyrosine phosphatase 1B (PTP1B), a validated target for Type II diabetes, which indicates that these analogs are worth further structural modification. Therefore, in this paper, a series of phidianidine derivatives were designed and rapidly synthesized with a function-oriented synthesis (FOS) strategy. Their inhibitory effects on PTP1B and T-cell protein tyrosine phosphatase (TCPTP) were evaluated, and several compounds displayed significant inhibitory potency and specific selectivity over PTP1B. The structure-activity relationship (SAR) and molecular docking analyses are also described. |
| WOS关键词 | PROTEIN-TYROSINE-PHOSPHATASE ; BIOLOGICAL EVALUATION ; INSULIN SENSITIVITY ; 1B INHIBITORS ; RESISTANCE ; MICE |
| 资助项目 | Natural Science Foundation of China[41676073] ; Natural Science Foundation of China[81520108028] ; Natural Science Foundation of China[81603022] ; NSFC-Shandong Joint Fund for Marine Science Research Centers[U1606403] ; Chinese Academy of Sciences[16PJ1410600] ; Chinese Academy of Sciences[2016258] ; China Association for Science and Technology[2016QNRC001] ; SA-SIBS Scholarship Program[00000000] ; SKLDR/SIMM Projects[SIMM 1705ZZ-01] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000428510200023 |
| 出版者 | MDPI |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279860]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物发现与设计中心 天然药物化学研究室 分析化学研究室 |
| 通讯作者 | Li, Xu-Wen; Guo, Yue-Wei |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Materia Med, State Key Lab Drug Res, 555 Zu Chong Zhi Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China; 2.Univ Sci & Technol China, Nano Sci & Technol Inst, 166 Ren Ai Rd, Suzhou 215123, Peoples R China; 3.Qingdao Natl Lab Marine Sci & Technol, Open Studio Druggabil Res Marine Nat Prod, 1 Wenhai Rd, Qingdao 266237, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Jin,Chen, Yu,Li, Jing-Ya,et al. Function-Oriented Synthesis of Marine Phidianidine Derivatives as Potential PTP1B Inhibitors with Specific Selectivity[J]. MARINE DRUGS,2018,16(3). |
| APA | Liu, Jin.,Chen, Yu.,Li, Jing-Ya.,Luo, Cheng.,Li, Jia.,...&Guo, Yue-Wei.(2018).Function-Oriented Synthesis of Marine Phidianidine Derivatives as Potential PTP1B Inhibitors with Specific Selectivity.MARINE DRUGS,16(3). |
| MLA | Liu, Jin,et al."Function-Oriented Synthesis of Marine Phidianidine Derivatives as Potential PTP1B Inhibitors with Specific Selectivity".MARINE DRUGS 16.3(2018). |
入库方式： OAI收割
来源：上海药物研究所
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