81555-97-7Relevant academic research and scientific papers
Synthesis, biological evaluation and molecular docking studies of novel 2-(1,3,4-oxadiazol-2-ylthio)-1-phenylethanone derivatives
Zhang, Li-Rong,Liu, Zhi-Jun,Zhang, Hui,Sun, Jian,Luo, Yin,Zhao, Ting-Ting,Gong, Hai-Bin,Zhu, Hai-Liang
, p. 3615 - 3621 (2012/07/27)
In present study, a series of new 2-(1,3,4-oxadiazol-2-ylthio)-1- phenylethanone derivatives (6a-6x) as potential focal adhesion kinase (FAK) inhibitors were synthesized. The bioassay assays demonstrated that compound 6i showed the most potent activity, which inhibited the growth of MCF-7 and A431 cell lines with IC50 values of 140 ± 10 nM and 10 ± 1 nM, respectively. Compound 6i also exhibited significant FAK inhibitory activity (IC50 = 20 ± 1 nM). Docking simulation was performed to position compound 6i into the active site of FAK to determine the probable binding model.
Synthesis and biological activity of some isoniazid based 1,3,4-oxadiazole derivatives
Khan,Chawla, Gita,Mueed, M. Asad
, p. 1302 - 1305 (2007/10/03)
1,3,4-Oxadiazole and isoniazid moieties are important because of their versatile biological actions. In the present studies, the oxadiazole system has been built with the isoniazid moiety and a few compounds in this series have been synthesised and their
The reaction of 5-aryl-(hetaryl)-2-aroylmethylthio-1,3,4-oxadiazoles with aryldiazonium tetrafluoroborates
Krasovsky,Andrushko,Demchenko
, p. 496 - 499 (2007/10/03)
5-Aryl(hetaryl)-2-aroylmethylthio-1,3,4-oxadiazoles behave as CH acids and readily react with aryldiazonium tetrafluoroborates at the active methylene group to give azo coupling products. The spectroscopic properties of the compounds synthesized have been
Ring Transformation of 1,3,4-Oxadiazole to s-Triazole-Fused Heterocycles. New Synthetic Route for Thiazolo-s-triazole and 7H-s-Triazolothiadiazine
Sasaki, Tadashi,Ito, Eikoh,Shimizu, Ikuo
, p. 2757 - 2760 (2007/10/02)
s-Triazole-fused heterocycles have been synthesized by an intramolecular transformation of some 1,3,4-oxadiazole ketones with ammonia or hydrazine.The α- ketone 2m gave thiazolo-s-triazole (4m), accompanied by a small amount of the hydrazide 9m on treatment with ammonium acetate in acetic acid.Similar treatment of ketones 2a and 2b afforded only the hydrazides 9a and 9b, respectively.Ketones 2a-n reacted with hydrazine hydrate in acetic acid to give 7H-s-triazolothiadiazines 5a-n.However, ketones 2o-q, with substituents α to the carbonyl group, could not be converted to the corresponding fused-ring systems.Mechanisms for these transformations are proposed.
