当前位置: X-MOL 学术J. Chem. Res. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis and biological evaluation of novel 6-alkoxy-3-aryl-[1,2,4]triazolo[4,3-b][1,2,4,5] tetrazines
Journal of Chemical Research ( IF 1.0 ) Pub Date : 2019-07-15 , DOI: 10.1177/1747519819861865
Run-Jie Shi 1 , Zhen-Zhen Yang 1 , Ye-Tao Gao 1 , Wen-Jin Cai 1 , Can Ye 1 , Feng Xu 1 , John Wang 2
Affiliation  

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 π–π 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.

中文翻译:

新型6-烷氧基-3-芳基-[1,2,4]三唑并[4,3-b][1,2,4,5]四嗪的合成与生物学评价

合成了一系列 6-烷氧基-3-芳基-[1,2,4] 三唑并 [4,3-b][1,2,4,5] 四嗪衍生物并评估了它们的抗肿瘤活性。这些化合物对 A549、Bewo 和 MCF-7 细胞表现出有效的抗增殖活性。进行分子对接研究抑制剂-c-Met激酶相互作用,结果表明6-乙氧基-3-苯乙基-[1,2,4]三唑并[4,3-b][1,2,4, 5] 四嗪通过两个氢键和一个 π-π 相互作用与 c-Met 激酶有效结合。基于这些初步结果,认为具有强抑制活性的化合物 6-乙氧基-3-苯乙基-[1,2,4]三唑并[4,3-b][1,2,4,5]四嗪可能是一种潜在的抗癌剂。
更新日期:2019-07-15
down
wechat
bug