We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Structure-Based Discovery of a Series of 5H-Pyrrolo[2,3-b]pyrazine FGFR Kinase Inhibitors.
- Authors
Jiang, Alan; Liu, Qiufeng; Wang, Ruifeng; Wei, Peng; Dai, Yang; Wang, Xin; Xu, Yechun; Ma, Yuchi; Ai, Jing; Shen, Jingkang; Ding, Jian; Xiong, Bing
- Abstract
Fibroblast growth factor receptors (FGFRs), a subfamily of receptor tyrosine kinases, are aberrant in various cancer types, and considered to be promising targets for cancer therapy. We started with a weak-active compound that was identified from our internal hepatocyte growth factor receptor (also called c-Met) inhibitor project, and optimized it with the guidance of a co-crystal structure of compound 8 with FGFR1. Through rational design, synthesis, and the biological evaluation of a series of 5H-pyrrolo[2,3-b]pyrazine derivatives, we discovered several potent FGFR kinase inhibitors. Among them, compound 13 displayed high selectivity and favorable metabolic properties, demonstrating a promising lead for further development.
- Publication
Molecules, 2018, Vol 23, Issue 3, p698
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules23030698