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Open AccessArticle

Discovery and Biological Evaluation of a Series of Pyrrolo[2,3-b]pyrazines as Novel FGFR Inhibitors

1
School of Pharmaceutical Sciences, Binzhou Medical University, Yantai 264003, Shandong, China
2
Division of Anti-Tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China
3
Department of Medicinal Chemistry, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China
4
Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China
*
Authors to whom correspondence should be addressed.
Academic Editors: Pierre Koch and Stefan Laufer
Molecules 2017, 22(4), 583; https://doi.org/10.3390/molecules22040583
Received: 26 January 2017 / Revised: 31 March 2017 / Accepted: 3 April 2017 / Published: 5 April 2017
(This article belongs to the Special Issue Kinase Inhibitors)
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 project, 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. View Full-Text
Keywords: FGFR1; inhibitor; kinase inhibitor; pyrazine; hinge binder FGFR1; inhibitor; kinase inhibitor; pyrazine; hinge binder
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MDPI and ACS Style

Zhang, Y.; Liu, H.; Zhang, Z.; Wang, R.; Liu, T.; Wang, C.; Ma, Y.; Ai, J.; Zhao, D.; Shen, J.; Xiong, B. Discovery and Biological Evaluation of a Series of Pyrrolo[2,3-b]pyrazines as Novel FGFR Inhibitors. Molecules 2017, 22, 583.

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