Discovery and Biological Evaluation of a Series of Pyrrolo[2,3-b]pyrazines as Novel FGFR Inhibitors
AbstractAbnormality 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
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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.
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(4):583.Chicago/Turabian Style
Zhang, Yan; Liu, Hongchun; Zhang, Zhen; Wang, Ruifeng; Liu, Tongchao; Wang, Chaoyun; Ma, Yuchi; Ai, Jing; Zhao, Dongmei; Shen, Jingkang; Xiong, Bing. 2017. "Discovery and Biological Evaluation of a Series of Pyrrolo[2,3-b]pyrazines as Novel FGFR Inhibitors." Molecules 22, no. 4: 583.
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