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

DOI: 10.1021/acs.jmedchem.8b01045

Source and publish data:

Journal of Medicinal Chemistry p. 7977 - 7990 (2018)

Update date:2022-07-29

Topics:

Authors:

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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Article abstract of DOI:10.1021/acs.jmedchem.8b01045

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, ti

Full text of DOI:10.1021/acs.jmedchem.8b01045

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