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Selective non-zinc binding MMP-2 inhibitors: Novel benzamide Ilomastat analogs with anti-tumor metastasis 期刊论文

编号：

35218c3e-c215-4f7a-afcf-7ef3097cef67
作者：

Song, Jiao^[1];Peng, Peng^[1];Chang, Jun(昌军)^[1]Liu, MingMing(刘明明)^[2]Yu, JianMing(于建明)^[1]Zhou, Lu(周璐)*^[2]Sun, Xun(孙逊)*^[1,3]
地址：

[1]Fudan Univ, Sch Pharm, Dept Nat Prod Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China;
[2]Fudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China;
[3]Shanghai Key Lab Clin Geriatr Med, 221 West Yanan Rd, Shanghai 200040, Peoples R China
语种：

English
期刊：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS ISSN：0960-894X 2016 年 26 卷 9 期 (2174 - 2178) ; MAY 1
收录：
关键词：

MMP-2 and MMP-9 Ilomastat analogs Benzamide groups Enzyme inhibition Non-zinc binding HEY cell invasion
摘要：

Novel Ilomastat analogs with substituted benzamide groups, instead of hydroxamic acid groups, were designed, synthesized and evaluated against MMP-2 and MMP-9. Among these analogs, the most potent compound 10a exhibited potent inhibitory activity against MMP-2 with IC50 value of 0.19 nM, which is 5 times more potent than that of Ilomastat (IC50 = 0.94 nM). Importantly, 10a exhibited more than 8300 fold selectivity for MMP-2 versus MMP-9 (IC50 = 1.58 mu M). Molecular docking studies showed that 10a bond to the catalytic active pocket of MMP-2 by a non-zinc-chelating mechanism which was different from that of Ilomastat. Furthermore, the invasion assay showed that 10a was effective in reducing HEY cells invasion at 84.6% in 50 mu M concentration. For 10a, the pharmacokinetic properties had been improved and especially the more desirable t(1/2z) was achieved compared with these of the lead compound Ilomastat. (C) 2016 Elsevier Ltd. All rights reserved.
推荐引用方式
GB/T 7714：

Song Jiao,Peng Peng,Chang Jun, et al. Selective non-zinc binding MMP-2 inhibitors: Novel benzamide Ilomastat analogs with anti-tumor metastasis [J].BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2016,26(9):2174-2178.
APA：

Song Jiao,Peng Peng,Chang Jun,Liu Ming-Ming,&Sun Xun.(2016).Selective non-zinc binding MMP-2 inhibitors: Novel benzamide Ilomastat analogs with anti-tumor metastasis .BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,26(9):2174-2178.
MLA：

Song Jiao, et al. "Selective non-zinc binding MMP-2 inhibitors: Novel benzamide Ilomastat analogs with anti-tumor metastasis" .BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 26,9(2016):2174-2178.

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