Discovery and Evaluation of Pyrazolo[3,4-d]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor

[Image: see text] The identification and lead optimization of a series of pyrazolo[3,4-d]pyridazinone derivatives are described as a novel class of potent irreversible BTK inhibitors, resulting in the discovery of compound 8. Compound 8 exhibited high potency against BTK kinase and acceptable PK pro...

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Udgivet i:ACS Med Chem Lett
Main Authors: Zhang, Xuejun, Sheng, Xijun, Shen, Jie, Zhang, Shoubo, Sun, Wenjie, Shen, Chunli, Li, Yi, Wang, Jun, Lv, Huqiang, Cui, Minghui, Zhu, Yuchuan, Huang, Lei, Hao, Dongling, Qi, Zhibo, Sun, Guanglong, Mao, Weifeng, Pan, Yan, Shen, Liang, Li, Xin, Hu, Guoping, Gong, Zhen, Han, Shuhua, Li, Jian, Chen, Shuhui, Tu, Ronghua, Wang, Xuehai, Wu, Chengde
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2019
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7549109/
https://ncbi.nlm.nih.gov/pubmed/33062165
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00395
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