Version 1
: Received: 30 March 2017 / Approved: 30 March 2017 / Online: 30 March 2017 (04:13:45 CEST)
How to cite:
yan, Z.; 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. Preprints2017, 2017030215. https://doi.org/10.20944/preprints201703.0215.v1.
yan, Z.; 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. Preprints 2017, 2017030215. https://doi.org/10.20944/preprints201703.0215.v1.
Cite as:
yan, Z.; 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. Preprints2017, 2017030215. https://doi.org/10.20944/preprints201703.0215.v1.
yan, Z.; 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. Preprints 2017, 2017030215. https://doi.org/10.20944/preprints201703.0215.v1.
Abstract
Abnormality of fibroblast growth factor receptors (FGFRs) mediated signaling pathways were frequently found in various human malignancies, making FGFRs hot targets for cancer treatment. To address the consistent need of new chemotype of FGFR inhibitors, here, we started with a hit structure identified from our internal 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 believed that our findings can benefit others to further develop selective FGFR inhibitors.
Keywords
FGFR1; inhibitor; kinase inhibitor; pyrazine; hinge binder
Subject
Medicine and Pharmacology, Oncology and Oncogenics
Copyright:
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.
