Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors

被引：13

作者：

Dong, Yuhong ^{[1
]}

Hu, Hao ^{[1
]}

Sun, Yuwei ^{[1
]}

Qin, Mingze ^{[1
]}

Gong, Ping ^{[1
]}

Hou, Yunlei ^{[1
]}

Zhao, Yanfang ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Key Lab Struct Based Drug Design & Discovery, Minist Educ, 103 Wenhua Rd, Shenyang 110016, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2020年 / 30卷 / 23期

基金：

中国国家自然科学基金;

关键词：

c-Met; HDAC; Design; Synthesis; Antitumor activity; HISTONE DEACETYLASE INHIBITORS; 4-PHENOXYQUINOLINE DERIVATIVES; MULTITARGET THERAPEUTICS; MULTIPLE LIGANDS; CANCER; MET; POLYPHARMACOLOGY; RECEPTOR; MOIETY;

D O I：

10.1016/j.bmcl.2020.127610

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this work three novel series of c-Met/HDAC bifunctional inhibitors were designed and synthesized by merging pharmacophores of c-Met and HDAC inhibitors. The most potent compound 11j inhibited c-Met kinase and HDAC1 with IC50 values of 21.44 and 45.22 nM, respectively. In addition, 11j showed efficient antiproliferative activities against both MCF-7 and A549 cells with greater potency than the reference drug SAHA and Cabozantinib. This work may lay the foundation for developing novel dual c-Met/HDAC inhibitors as potential anticancer therapeutics.

引用

页数：7

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