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Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-alpha Motif Kinase (ZAK) Inhibitors
Chang, Yu1; Lu, Xiaoyun2; Shibu, Marthandam Asokan3; Dai, Yi-Bo4; Luo, Jinfeng5; Zhang, Yan5; Li, Yingjun5; Zhao, Peng4; Zhang, Zhang5; Xu, Yong5; Tu, Zheng-Chao5; Zhang, Qing-Wen1; Yun, Cai-Hong4; Huang, Chih-Yang3; Ding, Ke2
2017-07-13
Source PublicationJOURNAL OF MEDICINAL CHEMISTRY
ISSN0022-2623
Volume60Issue:13Pages:5927-5932
Abstract

A series of N-(3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)bentenesulfonamides were designed as the first class of highly selective ZAK inhibitors. The representative compound 3h strongly inhibits the kinase activity of ZAK with an IC50 of 3.3 nM and dose-dependently suppresses the activation of ZAK downstream signals in vitro and in vivo, while it is significantly less potent for the majority of 403 nonmutated kinases evaluated. Compound 3h also exhibits orally therapeutic effects on cardiac hypertrophy in a spontaneous hypertensive rat model.

DOI10.1021/acs.jmedchem.7b00572
URLView the original
Indexed BySCI ; IC
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000405764900044
PublisherAMER CHEMICAL SOC
The Source to ArticleWOS
Fulltext Access
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Cited Times [WOS]:7   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China
2.School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China
3.Graduate Institute of Basic Medical Science, China Medical University, Taichung, Taiwan; Department of Health and Nutrition Biotechnology, Asia University, Taichung, Taiwan, China
4.Institute of Systems Biomedicine, Department of Biophysics and Beijing Key Laboratory of Tumor Systems Biology, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, China
5.Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, 190 Kaiyuan Avenue, Guangzhou 510530, China
First Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Chang, Yu,Lu, Xiaoyun,Shibu, Marthandam Asokan,et al. Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-alpha Motif Kinase (ZAK) Inhibitors[J]. JOURNAL OF MEDICINAL CHEMISTRY,2017,60(13):5927-5932.
APA Chang, Yu.,Lu, Xiaoyun.,Shibu, Marthandam Asokan.,Dai, Yi-Bo.,Luo, Jinfeng.,...&Ding, Ke.(2017).Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-alpha Motif Kinase (ZAK) Inhibitors.JOURNAL OF MEDICINAL CHEMISTRY,60(13),5927-5932.
MLA Chang, Yu,et al."Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-alpha Motif Kinase (ZAK) Inhibitors".JOURNAL OF MEDICINAL CHEMISTRY 60.13(2017):5927-5932.
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