54997-99-8Relevant articles and documents
Benzimidazole compound, preparation method thereof and application of the benzimidazole compound in preparation of ferroptosis inhibitor
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Paragraph 0066; 0070-0074; 0076, (2021/06/13)
The invention discloses a benzimidazole compound, a preparation method thereof and application of the benzimidazole compound in preparation of a ferroptosis inhibitor. The benzimidazole compound has a structure as shown in a formula (I) or a formula (II)
Discovery of 3-(5′-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation
Yan, Wei,Wang, Xinyi,Dai, Yang,Zhao, Bin,Yang, Xinying,Fan, Jun,Gao, Yinglei,Meng, Fanwang,Wang, Yuming,Luo, Cheng,Ai, Jing,Geng, Meiyu,Duan, Wenhu
supporting information, p. 6690 - 6708 (2016/08/06)
Fibroblast growth factor receptor (FGFR) represents an attractive oncology target for cancer therapy in view of its critical role in promoting cancer formation and progression, as well as causing resistance to approved therapies. In this article, we describe the identification of the potent pan-FGFR inhibitor (R)-21c (FGFR1-4 IC50 values of 0.9, 2.0, 2.0, and 6.1 nM, respectively). Compound (R)-21c exhibited excellent in vitro inhibitory activity against a panel of FGFR-amplified cell lines. Western blot analysis demonstrated that (R)-21c suppressed FGF/FGFR and downstream signaling pathways at nanomolar concentrations. Moreover, (R)-21c provided nearly complete inhibition of tumor growth (96.9% TGI) in NCI-H1581 (FGFR1-amplified) xenograft mice model at the dose of 10 mg/kg/qd via oral administration.
HETEROCYCLIC KINASE INHIBITORS
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Page 255, (2010/02/08)
Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.