623901-01-9Relevant academic research and scientific papers
Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia
Wang, Qiang,Liu, Feiyang,Qi, Shuang,Qi, Ziping,Yan, Xiao-E.,Wang, Beilei,Wang, Aoli,Wang, Wei,Chen, Cheng,Liu, Xiaochuan,Jiang, Zongru,Hu, Zhenquan,Wang, Li,Wang, Wenchao,Ren, Tao,Zhang, Shanchun,Yun, Cai-Hong,Liu, Qingsong,Liu, Jing
, p. 366 - 384 (2018/03/21)
Through exploration of the non-highly conserved allosteric hydrophobic pocket generated by DFG-out shifting in the inactive conformation, we discovered a highly selective type II PDGFRα kinase inhibitor 15i (CHMFL-PDGFRα-159), which exhibited strong poten
Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors
Lü, Shuang,Luo, Qun,Hao, Xiang,Li, Xianchan,Ji, Liyun,Zheng, Wei,Wang, Fuyi
experimental part, p. 6964 - 6968 (2012/01/05)
Six analogs of imatinib, an Abl kinase inhibitor clinically used as a first-line therapeutic agent for chronic myeloid leukaemia (CML), have been synthesized and characterized. And their potency as Abl kinase inhibitors have been screened by a robust virt
Optimization of novel combi-molecules: Identification of balanced and mixed bcr-abl/DNA targeting properties
Rachid, Zakaria,Katsoulas, Athanasia,Williams, Christopher,Larroque, Anne-Laure,McNamee, James,Jean-Claude, Bertrand J.
, p. 4248 - 4253 (2008/02/09)
Steps toward the identification of combi-molecules with strong abl tyrosine kinase (TK) inhibitory property and significant DNA damaging potential are described. The optimized combi-molecule 13a was shown to induce approximately twofold stronger abl TK in
Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase
Rachid, Zakaria,Katsoulas, Athanasia,Brahimi, Fouad,Jean-Claude, Bertrand Jacques
, p. 3297 - 3300 (2007/10/03)
The synthesis and abl tyrosine kinase inhibitory activities of alkyltriazenes conjugated to phenylaminopyrimidines are described. Significant abl inhibitory activities were observed only when a benzamido spacer was inserted between the 1,2,3-triazene chai
