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

Autor:	Shi Lei, Can Ye, Shi-Jie Zhang, Zhen-Zhen Yang, Zhong-Lu Ke, Feng Xu, Qidong Yan, Xiaoyu Wu
Rok vydání:	2020
Předmět:	chemistry.chemical_compound Tetrazine Stereochemistry Chemistry Triazole Tumor cells General Chemistry Biological evaluation
Zdroj:	Journal of Chemical Research. 44:543-550
ISSN:	2047-6507 1747-5198
DOI:	10.1177/1747519820911278
Popis:	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 1H NMR, 13C NMR, MS, and elemental analysis. Antitumor experiments indicated that some compounds exhibited significant inhibition activities against A549 and Bewo. Especially, the IC50 values of 5f (12 μM), 5h (7.1 μM), 6a (8.4 μM), and 6d (9.2 μM) demonstrated better antitumor activities against A549 than the positive agent cisplatin (13.3 μM), and the IC50 value of 6a (5.2 μM) exhibited better antitumor activity against Bewo than cisplatin (7.7 μM).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::eba06b91ba86094931f31da6399e2d07 https://doi.org/10.1177/1747519820911278 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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