900506-32-3Relevant academic research and scientific papers
Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases
McBride, Christopher M.,Renhowe, Paul A.,Heise, Carla,Jansen, Johanna M.,Lapointe, Gena,Ma, Sylvia,Pineda, Ramon,Vora, Jayesh,Wiesmann, Marion,Shafer, Cynthia M.
, p. 3595 - 3599 (2006)
3-Benzimidazol-2-yl-1H-indazole analogs were developed as inhibitors of receptor tyrosine kinases (RTK). The synthesis and SAR of this series is reported.
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.
3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors
McBride, Christopher M.,Renhowe, Paul A.,Gesner, Thomas G.,Jansen, Johanna M.,Lin, Julie,Ma, Sylvia,Zhou, Yasheen,Shafer, Cynthia M.
, p. 3789 - 3792 (2008/12/23)
The 3-benzimidazol-2-yl-1H-indazole scaffold was developed as an alternate scaffold for our receptor tyrosine kinase (RTK) inhibitor program. In exploring the SAR of this series, it was discovered that a subset of these compounds potently inhibit the enzy
