1139573-82-2Relevant academic research and scientific papers
Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors
Fan, Jun,Dai, Yang,Shao, Jingwei,Peng, Xia,Wang, Chen,Cao, Sufen,Zhao, Bin,Ai, Jing,Geng, Meiyu,Duan, Wenhu
, p. 2594 - 2599 (2016)
Fibroblast growth factor receptors (FGFRs) are important oncology targets due to the dysregulation of this signaling pathway in a wide variety of human cancers. We identified a series of pyrazolylaminoquinazoline derivatives as potent FGFR inhibitors with low nanomolar potency. The representative compound 29 strongly inhibited FGFR1-3 kinase activity and suppressed FGFR signaling transduction in FGFR-addicted cancer cells; FGFRs-driven cell proliferation was also strongly inhibited regardless of mechanistic complexity implicated in FGFR activation, which further confirmed that 29 was a potent pan-FGFR inhibitor. The flexibility of our structure offered the potential to preserve good affinity for mutant FGFR, which is important for developing TKIs with long-term efficacy.
GLYCOGEN PHOSPHORYLASE INHIBITOR COMPOUND AND PHARMACEUTICAL COMPOSITION THEREOF
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Page/Page column 7-8; 15, (2009/05/29)
This invention relates to a novel compound which is a glycogen phosphorylase inhibitor and its use in the treatment of diabetes and other conditions associated therewith. The invention further relates to a pharmaceutical composition containing the compoun
