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Molecules 2017, 22(4), 583; doi:10.3390/molecules22040583

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
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)
View Full-Text   |   Download PDF [6360 KB, uploaded 7 April 2017]   |  

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 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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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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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