773071-76-4Relevant 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
supporting information, p. 2594 - 2599 (2016/05/09)
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.
The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer
Lippa, Blaise,Kauffman, Goss S.,Arcari, Joel,Kwan, Tricia,Chen, Jinshan,Hungerford, William,Bhattacharya, Samit,Zhao, Xumiao,Williams, Courtney,Xiao, Jun,Pustilnik, Leslie,Su, Chunyan,Moyer, James D.,Ma, Ling,Campbell, Mary,Steyn, Stefanus
, p. 3081 - 3086 (2008/02/03)
The synthesis and biological evaluation of potent and selective inhibitors of the erbB2 kinase is presented. Based on the 4-anilinoquinazoline chemotype, the syntheses of several new series of erbB2 inhibitors are described with quinazoline and pyrido[4,3
