Synthesis, Activity Evaluation, and Molecular Docking of 3‐Quinolin(one)ly‐[1,2,4]triazolo[4,3‐ b ][1,2,4,5]tetrazine Derivatives as c‐Met Inhibitors

ChemMedChem 2026 Open access

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Authors: Yang Zhenzhen, Feng Xu, Guan Wang, Yan Ran, Jian Wang, Jiaxin Teng, Yanghong Lv, Zhelin Fang, Yutong Ye, Xinkai Ye, Yijing Zhou, Weiqiang Yang
+1 more Jianbo Yan
DOI: 10.1002/cmdc.202501008
Cited by: 1
References: 13

Abstract

Two series of [1,2,4]triazolo[4,3‐ b ][1,2,4,5]tetrazine derivatives have been synthesized and evaluated for their antitumor activities. These compounds exhibit potent antiproliferative activities against A549 and H460 cells and c‐Met kinase inhibitory activities. Five compounds are highly effective against A549 and H460 cells with IC 50 values in 2.97–16.50 μM (the mean ± SD value of three independent determinations). Molecular docking is further performed to study the inhibitor–c‐Met kinase interactions, and the results show that compound 3a is potently bound to the c‐Met kinase with three hydrogen bonds, one π‐‐‐π, and one CH‐‐‐π interactions. Based on the preliminary results, it is deduced that compound 3a with potent c‐Met kinase inhibitory activity may be a potential anticancer agent.

Fields of Study & Subjects

Click Chemistry and Applications Liver physiology and pathology Energetic Materials and Combustion

Publication details

Journal / source
ChemMedChem
Publisher
Wiley
Volume
21
Issue
2
Pages
e202501008–e202501008
Publication date
1 January 2026
Language
EN