1432017-45-2Relevant academic research and scientific papers
Synthesis and identification of 2,4-bisanilinopyrimidines bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential Aurora A inhibitors
Sang, Chun-Yan,Qin, Wen-Wen,Zhang, Xiu-Juan,Xu, Yu,Ma, You-Zhen,Wang, Xing-Rong,Hui, Ling,Chen, Shi-Wu
, p. 65 - 78 (2018/11/30)
The Aurora kinases are a family of serine/threonine kinases that interact with components of the mitotic apparatus and serve as potential therapeutic targets in oncology. Herein, we reported a series of 2,4-bisanilinopyrimidines bearing 2,2,6,6-tetramethylpiperidine-N-oxyl with selective inhibition of Aurora A in either enzymatic assays or cellular phenotypic assays, and displaying more potent anti-proliferation compared with that of VX-680. The most potent compound 10a forms better interaction with Aurora A than Aurora B in molecular docking. Mechanistic studies revealed that 10a disrupt the spindle formation, block the cell cycle progression in the G2/M phase and induce apoptosis in HeLa cell. These results suggested that the produced series of compounds are potential anticancer agents for further development as selective Aurora A inhibitors.
Aurora kinase A inhibitor and preparation and application thereof
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Paragraph 0027; 0028; 0029, (2017/07/12)
The invention discloses a novel stable nitroxide radical-marked aurora kinase A inhibitor and a preparation method and application thereof. The aurora kinase A inhibitor is N-(5-fluoro-4-o-chloroaniline-pyrimidin-2)-aminobenzoic acid 4-amino-2, 2, 6, 6-tetramethylpiperidyl oxynitride amide, or N-{5-fluoro-4-amino-(benzoyl o-chloroaniline)-pyrimidin-2}-aminobenzoic acid 4-amino-2, 2, 6, 6-tetramethylpiperidyl oxynitride amide. According to the preparation method, a target compound is prepared by performing a substitution reaction on 2, 4-dichloro-5-substituted-pyrimidine and aniline or p-aminobenzanilide and then 4-amino-2, 2, 6, 6-tetramethylpiperidyl nitrogen oxide. The aurora kinase A inhibitor is applied to preparation of anticancer medicines.
A facile route to steady redox-modulated nitroxide spin-labeled surfaces based on diazonium chemistry
Cougnon, Charles,Boisard, Severine,Cador, Olivier,Dias, Marylene,Levillain, Eric,Breton, Tony
, p. 4555 - 4557 (2013/06/05)
A TEMPO derivative was covalently grafted onto carbon and gold surfaces via the diazonium chemistry. The acid-dependent redox properties of the nitroxyl group were exploited to elaborate electro-switchable magnetic surfaces. ESR characterization demonstra
