Zhang Jian, Li Xiaoyang, Jiang Yuqi, Feng Jinhong, Li Xiaoguang, Zhang Yingjie, Xu Wenfang
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Wenhua Road, Ji'nan, Shandong 250012, China.
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Wenhua Road, Ji'nan, Shandong 250012, China.
Bioorg Med Chem. 2014 Jun 1;22(11):3055-64. doi: 10.1016/j.bmc.2013.12.025. Epub 2013 Dec 21.
A series of novel α-sulfonyl γ-(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.
设计、合成了一系列新型α-磺酰基γ-（甘氨酰氨基）脯氨酸拟肽衍生物，并对其抗基质金属蛋白酶-2（MMP-2）、氨肽酶N（APN）/CD13和组蛋白去乙酰化酶（HDACs）的活性进行了测定。结果表明，与APN和HDACs相比，所有化合物对MMP-2均表现出高度选择性抑制作用。还研究了一些化合物对SKOV3、HL60和A549细胞的抗增殖活性。与对照LY52相比，化合物12u在酶抑制试验和细胞试验中均具有优异的活性，可作为进一步开发MMP抑制剂的先导化合物。
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