Synthesis and LAR inhibition of 7-alkoxy analogues of illudalic acid
文献类型：期刊论文
| 作者 | Ling Q(凌青); Zhou YY(周越洋); Cai ZL(蔡正良); Zhang YH(张亚徽); Xiong B(熊兵) ; Ma LP(马兰萍); Wang X(王昕); Li X(李欣); Li J(李佳); Shen JK(沈竞康)
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| 刊名 | Acta Pharmaceutica Sinica
 |
| 出版日期 | 2010 |
| 卷号 | 45期号:11页码:1385-1397 |
| 关键词 | human leukocyte common antigen-related phosphatase illudalic acid inhibitor analogue structure-activity relationship |
| ISSN号 | 0513-4870 |
| 其他题名 | 7-烷基醚类illudalic acid类似物的合成及LAR抑制活性研究(英文) |
| 文献子类 | Article |
| 英文摘要 | To obtain higher potency and specificity,a series of 7-alkoxy analogues of illudalic acid was synthesized on the base of structure-activity relationship(SAR).All of these compounds exhibited submicromolar inhibition of the enzyme when tested against human leukocyte common antigen-related phosphatase(LAR)(for example, for 15e,IC50 = 180 nmol. L-1). They represent the most potent small-molecule inhibitors of LAR so far. These analogues also display excellent selectivity for LAR over other protein tyrosine phosphatases(PTPs) except for the highly homologous PTPsigma.The compound 15f is of 120-fold selectivity for LAR versus PTP-1B inhibition. The development of potent enzyme-specific inhibitors is so important that they may serve both as tools to study the role of LAR and as therapeutic agents for treatment of type II diabetes |
| 资助项目 | Hi-tech Research and Development Program of China[00000000] ; National Science & Technology Major Project"Key New Drug Creation and Manufacturing Program"of China[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4069709 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/267968]  |
| 专题 | 国家新药筛选中心 药物化学研究室 |
| 通讯作者 | Li J(李佳) |
| 作者单位 | 1.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, State Key Laboratory of Drug Research, Shanghai 201203, China.; 2.National Center for Drug Screening, Shanghai 201203, China. |
| 推荐引用方式 GB/T 7714 | Ling Q,Zhou YY,Cai ZL,et al. Synthesis and LAR inhibition of 7-alkoxy analogues of illudalic acid[J]. Acta Pharmaceutica Sinica,2010,45(11):1385-1397. |
| APA | 凌青.,周越洋.,蔡正良.,张亚徽.,熊兵.,...&沈竞康.(2010).Synthesis and LAR inhibition of 7-alkoxy analogues of illudalic acid.Acta Pharmaceutica Sinica,45(11),1385-1397. |
| MLA | 凌青,et al."Synthesis and LAR inhibition of 7-alkoxy analogues of illudalic acid".Acta Pharmaceutica Sinica 45.11(2010):1385-1397. |
入库方式： OAI收割
来源：上海药物研究所
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