1.
Hepatobiliary Pancreat Dis Int
; 20(5): 496-498, 2021 Oct.
Article
in English
| MEDLINE
| ID: mdl-34130912
2.
J Med Chem
; 60(13): 5927-5932, 2017 07 13.
Article
in English
| MEDLINE
| ID: mdl-28586211
ABSTRACT
A 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 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.