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

来源：

JOURNAL OF CHEMICAL RESEARCH | 2019年 / 43卷 / 9-10期

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

页码：313 / 318

页数：6

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