Design, synthesis and preliminary evaluation of 伪-sulfonyl 纬-(glycinyl-amino)proline peptidomimetics as matrix metalloproteinase inhibitors

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• 作者：Jian Zhang^a ; ^{zhangjian_3323@163.com" class="auth_mail} ; Xiaoyang Li^a ; Yuqi Jiang^a ; Jinhong Feng^b ; Xiaoguang Li^a ; Yingjie Zhang^a ; Wenfang Xu^a ; ^{wenfxu@gmail.com" class="auth_mail}
• 关键词：Matrix metalloproteinase-2 ; Aminopeptidase N ; HDACs ; Inhibitors ; Hyp-Gly derivatives ; Synthesis
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：1 June 2014
• 年：2014
• 卷：22
• 期：11
• 页码：3055-3064
• 全文大小：1152 K

文摘

A series of novel 伪-sulfonyl 纬-(glycinyl-amino)proline peptidomimetic derivatives were designed, synthesized and assayed for their activities against matrix metalloproteinase-2 (MMP-2), aminopeptidase N (APN)/CD13 and HDACs. The results indicated that all the compounds exhibited highly selective inhibition against MMP-2 as compared with APN and HDACs. The antiproliferative activities of some compounds against SKOV3, HL60 and A549 cells were also investigated. Comparing with the control LY52, compound 12u, with excellent activity both in the enzymatic inhibition assay and cell-based assay, could be used as lead compound for the further development of MMP inhibitors.