Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.

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ID: 1879
2019
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Abstract
ZAK is a new promising target for discovery of drugs with activity against antihypertrophic cardiomyopathy (HCM). A series of 1,2,3-triazole benzenesulfonamides were designed and synthesized as selective ZAK inhibitors. One of these compounds, 6p binds tightly to ZAK protein ( K = 8.0 nM) and potently suppresses the kinase function of ZAK with single-digit nM (IC = 4.0 nM) and exhibits excellent selectivity in a KINOMEscan screening platform against a panel of 403 wild-type kinases. This compound dose dependently blocks p38/GATA-4 and JNK/c-Jun signaling and demonstrates promising in vivo anti-HCM efficacy upon oral administration in a spontaneous hypertensive rat (SHR) model. Compound 6p may serve as a lead compound for new anti-HCM drug discovery.
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yang2019designjournal Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Yang, Jianzhang;Shibu, Marthandam Asokan;Kong, Lulu;Luo, Jinfeng;BadrealamKhan, Farheen;Huang, Yanhui;Tu, Zheng-Chao;Yun, Cai-Hong;Huang, Chih-Yang;Ding, Ke;Lu, Xiaoyun;
Journal Journal of medicinal chemistry
Year 2019
DOI
10.1021/acs.jmedchem.9b00664
URL
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