标题:Novel potent 2,5-pyrrolidinedione peptidomimetics as aminopeptidase N inhibitors. Design, synthesis and activity evaluation
作者:Li,Q.;Fang,H.;Wang,X.;Hu,G.;Wang,Q.;Xu,W.
作者机构:[Li, Q] Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Central South University, 172 Tongzipo Road, 410013 Changsha, Hu'nan, Ch 更多
通讯作者:Li, QB
通讯作者地址:[Li, QB]Cent S Univ, Sch Pharmaceut Sci, Dept Med Chem, 172 Tongzipo Rd, Changsha 410013, Hunan, Peoples R China.
来源:Bioorganic and Medicinal Chemistry Letters
出版年:2012
卷:22
期:2
页码:850-853
DOI:10.1016/j.bmcl.2011.12.048
关键词:2;5-Pyrrolidinedione;Aminopeptidase N;Anti-tumor;Peptidomimetics;Synthesis
摘要:A series of novel aminopeptidase N inhibitors with 2,5-pyrrolidinedione scaffold were chemically synthesized. Their preliminary biological activities in enzyme kinetics and cell assay in vitro and anti-metastasis profile in vivo were also evaluated. The results indicated that all the compounds displayed potent inhibitory activity against aminopeptidase N. Compound 8f inhibited aminopeptidase N activity with IC 50 value of 1.0 μM and displayed better activity profile in vivo than that of bestatin.
收录类别:SCOPUS;SCIE
WOS核心被引频次:6
Scopus被引频次:6
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84855669459&doi=10.1016%2fj.bmcl.2011.12.048&partnerID=40&md5=b57870ec72733e87896dd4f7b53467a4
TOP