Synthesis and biological evaluation of novel thiadiazole amides as potent Cdc25B and PTP1B inhibitors
文献类型：期刊论文
| 作者 | Li, Yingjun1; Yu, Yang1; Jin, Kun2; Gao, Lixin3; Luo, Tongchuan1; Sheng, Li3; Shao, Xin1; Li, Jia3
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2014-09-01 |
| 卷号 | 24期号:17页码:4125-4128 |
| 关键词 | Thiadiazole amides Cdc25B PTP1B Cancer Type-2 diabetes and obesity |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2014.07.055 |
| 文献子类 | Article |
| 英文摘要 | A series of novel thiadiazole amide derivatives have been synthesized and evaluated for inhibitory activities against Cdc25B and PTP1B. Most of them showed inhibitory activities against Cdc25B (IC50 = 1.18-8.01 mu g/mL) and PTP1B (IC50 = 0.85-8.75 mu g/mL), respectively. Moreover, compounds 5b and 4l were most potent with IC50 values of 1.18 and 0.85 mu g/mL for Cdc25B and PTP1B, respectively, compared with reference drugs Na3VO4 (IC50 = 0.93 mu g/mL) and oleanolic acid (IC50 = 0.85 mu g/mL). The results of selectivity experiments showed that the target compounds were selective inhibitors against PTP1B and Cdc25B. Enzyme kinetic experiments demonstrated that compound 5k was a specific inhibitor with the typical characteristics of a mixed inhibitor. (C) 2014 Elsevier Ltd. All rights reserved. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; MOLECULAR DOCKING ; DERIVATIVES ; DESIGN ; NAPHTHOQUINONE ; DISCOVERY ; AGENTS ; ACID |
| 资助项目 | National Science and Technology Major Projects for 'Major New Drugs Innovation and Development' of China[2012ZX09301001-004] ; National Science and Technology Major Projects for 'Major New Drugs Innovation and Development' of China[2013ZX09507002] ; National Natural Science Foundation of China[81125023] ; Shanghai Commission of Science and Technology of China[13DZ2290300] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000341339300011 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276920]  |
| 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 药物安全性评价中心 |
| 通讯作者 | Li, Yingjun |
| 作者单位 | 1.Liaoning Normal Univ, Coll Chem & Chem Engn, Dalian 116029, Peoples R China; 2.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116012, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Yingjun,Yu, Yang,Jin, Kun,et al. Synthesis and biological evaluation of novel thiadiazole amides as potent Cdc25B and PTP1B inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2014,24(17):4125-4128. |
| APA | Li, Yingjun.,Yu, Yang.,Jin, Kun.,Gao, Lixin.,Luo, Tongchuan.,...&Li, Jia.(2014).Synthesis and biological evaluation of novel thiadiazole amides as potent Cdc25B and PTP1B inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,24(17),4125-4128. |
| MLA | Li, Yingjun,et al."Synthesis and biological evaluation of novel thiadiazole amides as potent Cdc25B and PTP1B inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 24.17(2014):4125-4128. |
入库方式： OAI收割
来源：上海药物研究所
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