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- Title
Discovery and Biological Evaluation of a Series of Pyrrolo[2,3-b]pyrazines as Novel FGFR Inhibitors.
- Authors
Yan Zhang; Hongchun Liu; Zhen Zhang; Ruifeng Wang; Tongchao Liu; Chaoyun Wang; Yuchi Ma; Jing Ai; Dongmei Zhao; Jingkang Shen; Bing Xiong
- Abstract
Abnormality of fibroblast growth factor receptor (FGFR)-mediated signaling pathways were frequently found in various human malignancies, making FGFRs hot targets for cancer treatment. To address the consistent need for a new chemotype of FGFR inhibitors, here, we started with a hit structure identified from our internal hepatocyte growth factor receptor (also called c-Met) inhibitor projecţ and conducted a chemical optimization. After exploring three parts of the hit compound, we finally discovered a new series of pyrrolo[2,3-b]pyrazine FGFR inhibitors, which contain a novel scaffold and unique molecular shape. We believe that our findings can help others to further develop selective FGFR inhibitors.
- Subjects
FIBROBLAST growth factor receptors; PYRAZINE derivatives; CANCER treatment; GENE expression; HEPATOCYTE growth factor
- Publication
Molecules, 2017, Vol 22, Issue 4, p583
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules22040583