5089-08-7Relevant articles and documents
Design, synthesis, and biological activity of phenyl-pyrazole derivatives as BCR-ABL kinase inhibitors
Hu, Liming,Zheng, Yuyan,Li, Zhipeng,Wang, Yujie,Lv, Yongjuan,Qin, Xuemei,Zeng, Chengchu
, p. 3147 - 3152 (2015)
Abstract 4-(Pyridin-3-yl)-1H-pyrazol-1-yl-phenyl-3-benzamide derivatives have been proposed as new BCR-ABL tyrosine kinase inhibitors by using combinational strategies of scaffold hopping and conformational constraint. In the present study, a series of 4-
Imatinib derivative as well as preparation method and application thereof
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Paragraph 0043; 0044; 0045-0046, (2019/09/17)
The invention discloses an imatinib derivative. The chemical name of the imatinib derivative is (E)-1-(3,5-dibromobenzyl)-4-(4-methyl-3-(4-(pyridine-3-yl)pyrimidine-2-amino)phenyl)semicarbazide, and the structural formula of the derivative is shown in the description, wherein R is 3,5-dibromobenzyl. The invention further discloses a preparation method of the imatinib derivative. The preparation ofthe imatinib derivative with a new structure is disclosed and the derivative has certain antitumor activity; the preparation method of the compound is also disclosed, the reaction cost is low, the yield is high, the reaction process is simple and easy to control, and the preparation method is suitable for industrial production.
Design, synthesis, and biological activity of 4-(imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-phenylbenzamide derivatives as BCR–ABL kinase inhibitors
Hu, Liming,Cao, Tingting,Lv, Yongjuan,Ding, Yiming,Yang, Leifu,Zhang, Qiang,Guo, Mingzhou
supporting information, p. 5830 - 5835 (2016/11/25)
A series of 4-((pyrazolo[1,5-a]pyrimidin-6-yl)-1H-pyrazol-1-yl)phenyl-3-benzamide derivatives and 4-((imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-)phenyl-3-benzamide derivatives were designed, synthesized as new BCR–ABL tyrosine kinase inhibitors by using combinational strategies of scaffold hopping and conformational constraint. These new compounds were screened for BCR–ABL1 kinase inhibitory activity, and most of them appeared good inhibitory activity against BCR–ABL1 kinase. One of the most potent compounds 16a strongly suppressed BCR–ABL1 kinase with IC50value of 8.5 nM. The tested compounds 16a and 16i showed strong inhibitory activities against K562 with IC50value of less than 2 nM. Molecular docking studies indicated that these compounds fitted well with the active site of BCR–ABL1 protein. The results showed these inhibitors may serve as lead compounds for further developing new drugs targeted BCR–ABL kinase.