structure-based discovery of a series of 5h-pyrrolo[2,3-b]pyrazine fgfr kinase inhibitors

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ID: 128596
2018
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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.
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jiang2018moleculesstructure-based Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Alan Jiang, Qiufeng Liu, Ruifeng Wang, Peng Wei, Yang Dai, Xin Wang, Yechun Xu, Yuchi Ma, Jing Ai, Jingkang Shen, Jian Ding, Bing Xiong
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Journal Journal of ethnopharmacology
Year 2018
DOI
10.3390/molecules23030698
URL
http://www.mdpi.com/1420-3049/23/3/698
Keywords
Cancer 3-b]pyrazineorganic chemistry

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