- Design, synthesis, and biological activity of phenyl-pyrazole derivatives as BCR-ABL kinase inhibitors
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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-
- Hu, Liming,Zheng, Yuyan,Li, Zhipeng,Wang, Yujie,Lv, Yongjuan,Qin, Xuemei,Zeng, Chengchu
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- Synthesis and evaluation of indole-substituted N-heterocyclic carbene ligands
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Indole-substituted N-heterocyclic carbene ligands were synthesized and evaluated through both computational and experimental methods. The performances of medium-sized imidazolylidenes IIn3 and IIn4 were comparable to IPr in the Cu(I)-catalyzed carboxylation of organoboronic esters.
- Yan, Huan,Liu, Zhongxian,Tan, Kai,Ji, Ruigeng,Ye, Yingxin,Yan, Tingbing,Shen, Yuehai
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supporting information
(2020/10/05)
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- Imatinib derivative as well as preparation method and application thereof
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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.
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Paragraph 0043; 0044; 0045-0046
(2019/09/17)
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- Benzamide derivative, preparation and application
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The invention relates to a benzamide derivative expressed in the formula N-(3-(4-(3-imidazo[1,2-b]pyridazinyl)-1-pyraxolyl)-4-methyl phenyl), preparation and application and belongs to the field of medicinal chemistry. R1 represents -OCH3 or -F or -CF3 or
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Paragraph 0052 ; 0053 ; 0054 ; 0055 ; 0056
(2016/10/08)
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- 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
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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.
- Hu, Liming,Cao, Tingting,Lv, Yongjuan,Ding, Yiming,Yang, Leifu,Zhang, Qiang,Guo, Mingzhou
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supporting information
p. 5830 - 5835
(2016/11/25)
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- SYNTHESIS OF 4-NITRO-3,3,7-TRIMETHYL-2-(2-HYDROXYSTYRYL)INDOLENINES
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The previously unknown hydroxystyrylindolenines have been synthesized by the direct condensation of 4-nitro-2,3,3,7-tetramethylindolenine with substituted salicylaldehydes.The structure of the prepared compounds has been confirmed by spectroscopic investi
- Przhiyalgovskaya, N. M.,Manakova, I. V.,Kurkovskaya, L. N.,Suvorov, N. N.
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p. 290 - 292
(2007/10/02)
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- Process for producing 3-anilino-5-pyrazolones
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A process for producing a 3-anilino-5-pyrazolone which comprises reacting a β-anilino-β-alkoxy-acrylate with a hydrazine in the presence of a compound having a pKa of about 8 up to about 14.
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