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Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2-a]pyrazin-3-ylethynyl)-4-isopropyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2
[Image: see text] Discoidin-domain receptors 1 and 2 (DDR1 and DDR2) are new potential targets for anti-inflammatory-drug discovery. A series of heterocycloalkynylbenzimides were designed and optimized to coinhibit DDR1 and DDR2. One of the most promising compounds, 5n, tightly bound to DDR1 and DDR...
Autores principales: | Wang, Zhen, Zhang, Yali, Pinkas, Daniel M., Fox, Alice E., Luo, Jinfeng, Huang, Huocong, Cui, Shengyang, Xiang, Qiuping, Xu, Tingting, Xun, Qiuju, Zhu, Dongsheng, Tu, Zhengchao, Ren, Xiaomei, Brekken, Rolf A., Bullock, Alex N., Liang, Guang, Ding, Ke, Lu, Xiaoyun |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical
Society
2018
|
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6287892/ https://www.ncbi.nlm.nih.gov/pubmed/30075624 http://dx.doi.org/10.1021/acs.jmedchem.8b01045 |
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