623900-99-2Relevant academic research and scientific papers
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 (2007)
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
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
Phenylaminopyrimidine derivatives and methods of use
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, (2008/06/13)
The present invention relates to phenylaminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states such as cancers associated with tyrosine kinases, especially Bcr-Abl, to their use as medicaments and to their use in the manufacture of medicaments for use in the production of inhibition of tyrosine kinase reducing effects in warm-blooded animals such as humans.
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
