- Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors
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The structure-based design of 1, 2, 3, 4-tetrahydroisoquinoline derivatives as selective DDR1 inhibitors is reported. One of the representative compounds, 6j, binds to DDR1 with a Kd value of 4.7 nM and suppresses its kinase activity with an IC50 value of 9.4 nM, but it is significantly less potent for a panel of 400 nonmutated kinases. 6j also demonstrated reasonable pharmacokinetic properties and a promising oral therapeutic effect in a bleomycin-induced mouse pulmonary fibrosis model.
- Wang, Zhen,Bian, Huan,Bartual, Sergio G.,Du, Wenting,Luo, Jinfeng,Zhao, Hu,Zhang, Shasha,Mo, Cheng,Zhou, Yang,Xu, Yong,Tu, Zhengchao,Ren, Xiaomei,Lu, Xiaoyun,Brekken, Rolf A.,Yao, Libo,Bullock, Alex N.,Su, Jin,Ding, Ke
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supporting information
p. 5911 - 5916
(2016/07/06)
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- COMPOUNDS FOR TREATMENT OF NEURODEGENERATIVE DISEASES
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The present invention relates to a class of small molecule hydroxamic acid compounds capable of inhibiting histone deacetylases (HDACs). The present invention also relates to methods of preparation of hydroxamic acid HDAC inhibitor compounds of the invent
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Page/Page column 13; 29
(2010/02/14)
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