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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-α Motif Kinase (ZAK) Inhibitors
Chang Y.6; Lu X.5; Shibu M.A.4; Dai Y.-B.2; Luo J.3; Zhang Y.3; Li Y.3; Zhao P.2; Zhang Z.3; Xu Y.3; Tu Z.-C.3; Zhang Q.-W.6; Yun C.-H.2; Huang C.-Y.4; Ding K.5
2017-07-13
Source PublicationJournal of Medicinal Chemistry
ISSN15204804 00222623
Volume60Issue:13Pages:5927-5932
AbstractA series of N-(3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides were designed as the first class of highly selective ZAK inhibitors. The representative compound 3h strongly inhibits the kinase activity of ZAK with an IC 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
Language英語
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Cited Times [WOS]:4   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.Asia University Taiwan
2.Peking University
3.Chinese Academy of Sciences
4.China Medical University Taichung
5.Jinan University
6.Universidade de Macau
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GB/T 7714
Chang Y.,Lu X.,Shibu M.A.,et al. Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors[J]. Journal of Medicinal Chemistry,2017,60(13):5927-5932.
APA Chang Y..,Lu X..,Shibu M.A..,Dai Y.-B..,Luo J..,...&Ding K..(2017).Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.Journal of Medicinal Chemistry,60(13),5927-5932.
MLA Chang Y.,et al."Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors".Journal of Medicinal Chemistry 60.13(2017):5927-5932.
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