Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors

[Image: see text] 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 K(d) value of 4.7 nM and suppresses its kinase activity with an IC(50) value of 9.4 nM, but it is sign...

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Vydáno v:J Med Chem
Hlavní autoři: 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
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2016
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC5053573/
https://ncbi.nlm.nih.gov/pubmed/27219676
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b00140
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