Synthesis and biological evaluation of novel 6-alkoxy-3-aryl-[1,2,4]triazolo[4,3-b][1,2,4,5] tetrazines

被引:6
|
作者
Shi, Run-Jie [1 ]
Yang, Zhen-Zhen [1 ]
Gaol, Ye-Tao [1 ]
Cai, Wen-Jin [1 ]
Ye, Can [1 ]
Xu, Feng [1 ]
Wang, John [2 ]
机构
[1] Taizhou Vocat & Tech Coll, Pharmaceut Res Inst, Taizhou 318000, Peoples R China
[2] ImmuOn Therapeut, Nantong, Peoples R China
关键词
anticancer; c-Met; molecular docking; synthesis; tetrazines; triazoles; ANTITUMOR EVALUATION; ANTICANCER AGENTS; DERIVATIVES; SYSTEM; INHIBITORS; 3D-QSAR; UPDATE;
D O I
10.1177/1747519819861865
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of 6-alkoxy-3-aryl-[1,2,4]triazolo[4,3-b][1,2,4,5] tetrazine derivatives is synthesized and evaluated for their antitumor activities. These compounds exhibit potent antiproliferative activities against A549, Bewo, and MCF-7 cells. Molecular docking is performed to study the inhibitor-c-Met kinase interactions, and the results show that 6-ethoxyl-3-phenylethyl-[1,2,4]triazolo[4,3-b][1,2,4,5] tetrazine is potently bound to c-Met kinase with two hydrogen bonds and one pi-pi interaction. Based on these preliminary results, it is thought that compound 6-ethoxyl-3-phenylethyl-[1,2,4]triazolo[4,3-b][1,2,4,5] tetrazine with potent inhibitory activity may be a potential anticancer agent.
引用
收藏
页码:313 / 318
页数:6
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