77476-95-0Relevant articles and documents
Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl) benzamide derivatives as potent pan Bcr-Abl inhibitors including the threonine315←isoleucine315 mutant
Li, Yupeng,Shen, Mengjie,Zhang, Zhang,Luo, Jinfeng,Pan, Xiaofen,Lu, Xiaoyun,Long, Huoyou,Wen, Donghai,Zhang, Fengxiang,Leng, Fang,Li, Yingjun,Tu, Zhengchao,Ren, Xiaomei,Ding, Ke
, p. 10033 - 10046 (2013/01/16)
A series of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives were designed and synthesized as new Bcr-Abl inhibitors by using combinational strategies of bioisosteric replacement, scaffold hopping, and conformational constraint. The compounds displayed significant inhibition against a broad spectrum of Bcr-Abl mutants including the gatekeeper T315I and p-loop mutations, which are associated with disease progression in CML. The most potent compounds 6q and 6qo strongly inhibited the kinase activities of Bcr-AblWT and Bcr-AblT315I with IC50 values of 0.60, 0.36 and 1.12, 0.98 nM, respectively. They also potently suppressed the proliferation of K562, KU812 human CML cells, and a panel of murine Ba/F3 cells ectopically expressing either Bcr-AblWT or any of a panel of other Bcr-Abl mutants that have been shown to contribute to clinical acquired resistance, including Bcr-AblT315I, with IC50 values in low nanomolar ranges. These compounds may serve as lead compounds for further development of new Bcr-Abl inhibitors capable of overcoming clinical acquired resistance against imatinib.
BIARYL COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 168, (2011/04/13)
Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
Halogeno derivatives of isopropylamino pyrimidine and therapeutic use
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, (2008/06/13)
The invention relates to new isopropylamino pyrimidine halogeno derivatives of the formula: STR1 in which X represents a fluorine, a chlorine or a bromine atom. These compounds, when X stands for chlorine or bromine, are prepared by reacting, at room temperature and in stoichiometric proportions, 2-isopropylamino pyrimidine on the appropriate N-halogeno succinimide, in the presence of acetic acid.