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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, Yu; Lu, Xiaoyun; Shibu, Marthandam Asokan; Dai, Yi-Bo; Luo, Jinfeng; Zhang, Yan; Li, Yingjun; Zhao, Peng; Zhang, Zhang; Xu, Yong; Tu, Zheng-Chao; Zhang, Qing-Wen; Yun, Cai-Hong; Huang, Chih-Yang; Ding, Ke
2017-07-13
Source PublicationJOURNAL OF MEDICINAL CHEMISTRY
ISSN0022-2623
Volume60Issue:13Pages:5927-5932
AbstractA 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
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Cited Times [WOS]:4   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
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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