864770-82-1Relevant articles and documents
INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS
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, (2021/09/11)
The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer
Zhu, Wei,Chen, Hui,Wang, Yulan,Wang, Jiang,Peng, Xia,Chen, Xianjie,Gao, Yinglei,Li, Chunpu,He, Yulong,Ai, Jing,Geng, Meiyu,Zheng, Mingyue,Liu, Hong
, p. 6018 - 6035 (2017/08/02)
A novel series of pyridin-3-amine derivatives were designed, synthesized, and evaluated as multitargeted protein kinase inhibitors for the treatment of non-small cell lung cancer (NSCLC). Hit 1 was first disclosed by in silico screening against fibroblast
2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity
Lin, Hong,Yamashita, Dennis S.,Zeng, Jin,Xie, Ren,Wang, Wenyong,Nidarmarthy, Sirishkumar,Luengo, Juan I.,Rhodes, Nelson,Knick, Victoria B.,Choudhry, Anthony E.,Lai, Zhihong,Minthorn, Elisabeth A.,Strum, Susan L.,Wood, Edgar R.,Elkins, Patricia A.,Concha, Nestor O.,Heerding, Dirk A.
body text, p. 673 - 678 (2010/07/05)
2,3,5-Trisubstituted pyridines have been designed as potent AKT inhibitors that are selective against ROCK1 based on the comparison between AKT and ROCK1 structures. Substitution at the 2-position of the core pyridine is the key element to provide selectivity against ROCK1. An X-ray co-crystal structure of 9p in PKA supports the proposed rationale of ROCK1 selectivity.