64064-56-8Relevant articles and documents
Design, synthesis, and biological evaluation of pyridineamide derivatives containing a 1,2,3-triazole fragment as type II c-Met Inhibitors
Xiong, Hehua,Cheng, Jianxin,Zhang, Jianqing,Zhang, Qian,Xiao, Zhen,Zhang, Han,Tang, Qidong,Zheng, Pengwu
, (2020/01/13)
A series of 4-(pyridin-4-yloxy)benzamide derivatives containing a 1,2,3-triazole fragment were designed, synthesized, and their inhibitory activity against A549, HeLa, and MCF-7 cancer cell lines was evaluated. Most compounds exhibited moderate to potent antitumor activity against the three cell lines. Among them, the promising compound B26 showed stronger inhibitory activity than Golvatinib, with IC50 values of 3.22, 4.33, and 5.82 μM against A549, HeLa, and MCF-7 cell lines, respectively. The structure-activity relationships (SARs) demonstrated that the modification of the terminal benzene ring with a single electron-withdrawing substituent (fluorine atom) and the introduction of a pyridine amide chain with a strong hydrophilic group (morpholine) to the hinge region greatly improved the antitumor activity. Meanwhile, the optimal compound B26 showed potent biological activity in some pharmacological experiments in vitro, such as cell morphology study, dose-dependent test, kinase activity assay, and cell cycle experiment. Finally, the molecular docking simulation was performed to further explore the binding mode of compound B26 with c-Met.
Design, synthesis and biological evaluation of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment
Duan, Yongli,Tang, Qidong,Xiong, Hehua,Zhang, Han,Zhang, Jianqing,Zhang, Qian,Zheng, Pengwu
, (2020/03/23)
A series of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment were designed, synthesized, and evaluated for their biological activity. Most compounds showed effective inhibitory activity against cancer cell lines of A
Preparation and application of 2-pyridine carboxamide compound
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, (2019/12/25)
The invention relates to a 2-pyridine carboxamide derivative as shown in a formula I, and pharmaceutically acceptable salt, hydrate, solvate and prodrug thereof. Substituents R1, R2, X and Y have themeanings given in the description. The invention further relates to a compound in the general formula I, and the compound has the strong inhibition effect on FLT-3; the invention further relates to the applications of the compound, and the pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof to preparation of drugs for treating diseases caused by abnormal high expression of FLT-3kinase, especially the applications to preparation of drugs for treating and/or preventing cancers.