Synthesis, biological evaluation, and molecular docking of ((4-([1,2,4]triazolo[4,3-b][1,2,4,5]tetrazin-6-yl) piperazin-1-yl)methyl) benzohydrazide derivatives

被引:5
作者
Wu, Xiaoyu [1 ]
Xu, Feng [2 ]
Yang, Zhenzhen [2 ]
Ke, Zhonglu [2 ]
Shi, Lei [2 ]
Ye, Can [2 ]
Yan, Qidong [2 ]
Zhang, Shijie [3 ]
机构
[1] Taizhou Univ Hosp, Taizhou Cent Hosp, Lab Dept, Taizhou, Peoples R China
[2] Taizhou Vocat & Tech Coll, Biopharmaceut Res & Dev Ctr, Taizhou 318000, Peoples R China
[3] Zhejiang Chinese Med Univ, Acad Chinese Med Sci, Hangzhou, Peoples R China
关键词
anticancer; c-Met; molecular docking; synthesis; tetrazine; triazole; ANTITUMOR EVALUATION; MET RECEPTOR; RESISTANCE; GROWTH; INHIBITORS; CELLS; METASTASIS; DISCOVERY;
D O I
10.1177/1747519820911278
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of ((4-([1,2,4]triazolo[4,3-b][1,2,4,5] methyl) benzo-hydrazide derivatives was designed, synthesized, and evaluated for their inhibition activities against five tumor cells and c-Met kinase in vitro. These compounds were fully characterized by(1)H NMR,C-13 NMR, MS, and elemental analysis. Antitumor experiments indicated that some compounds exhibited significant inhibition activities against A549 and Bewo. Especially, the IC(50)values of5f(12 mu M),5h(7.1 mu M),6a(8.4 mu M), and6d(9.2 mu M) demonstrated better antitumor activities against A549 than the positive agent cisplatin (13.3 mu M), and the IC(50)value of6a(5.2 mu M) exhibited better antitumor activity against Bewo than cisplatin (7.7 mu M).
引用
收藏
页码:543 / 550
页数:8
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