25165-68-8Relevant academic research and scientific papers
INHIBITORS FOR THE TREATMENT OF CANCER AND RELATED METHODS
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Paragraph 0032; 0176, (2019/05/15)
Some embodiments of the invention include inventive compounds. Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutica
Organic optoelectronic functional material and application thereof
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Paragraph 0074-0076, (2019/01/06)
The invention belongs to the field of organic electroluminescent devices, and discloses an organic electroluminescent material containing a diquinolyl structure and application of the organic electroluminescent material. By using the organic electroluminescent material provided by the invention as an electron transport material, the produced device has good electron mobility and relatively-balanced current carrier transmission property, and the improvement efficiency of the device is facilitated. In addition, the organic electroluminescent material provided by the invention also can be furtherblended with a hole type main body material so as to form an exciplex; by using the exciplex as a co-subject material, the efficiency and the stability of the produced device are both improved obviously.
SELECTIVE PFKFB4 INHIBITORS FOR THE TREATMENT OF CANCER
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Page/Page column 61, (2016/11/14)
Methods and pharmaceutical compositions for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 4 (PFKFB4) and the treatment of cancer are described.
Discovery of 4-(4-(2-((5-Hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)(propyl) amino)ethyl)piperazin-1-yl)quinolin-8-ol and its analogues as highly potent dopamine D2/D3 agonists and as iron chelator: In vivo activity indicates potential application in symptomatic and neuroprotective therapy for Parkinson's disease
Ghoshs, Balaram,Antonio, Tamara,Reith, Maarten E. A.,Dutta, Aloke K.
experimental part, p. 2114 - 2125 (2010/08/20)
The role of iron in the pathogenesis of Parkinson's disease (PD) has been implicated strongly because of generation of oxidative stress leading to dopamine cell death. In our overall goal to develop bifunctional/multifunctional drugs, we designed dopamine D2/D3 agonist molecules with a capacity to bind to iron. Binding assays were carried out with HEK-293 cells expressing either D2 or D3 receptor with tritiated spiperone to evaluate inhibition constants (K i). Functional activity of selected compounds was carried out with GTPyS binding assay. SAR results identified compounds (+)-19a and (-)-19b as two potent agonists for both D2 and D3 receptors (EC50 (GTPyS); D2 = 4.51 and 1.69 nM and D3 = 1.58 and 0.74 nM for (-)-19b and (+)-19a, respectively). In vitro complexation studies with 19b demonstrated efficient chelation with iron. Furthermore, the deoxyribose assay with 19b demonstrated potent antioxidant activity. In PD animal model study, (-)-19b exhibited potent in vivo activity in reversing locomotor activity in reserpinized rats and also in producing potent rotational activity in 6-OHDA lesioned rats. This reports initial development of unique lead molecules that might find potential use in symptomatic and neuroprotective treatment of PD.
Direct C-3-alkenylation of quinolones via palladium-catalyzed C-H functionalization
Li, Mingzong,Li, Liangxi,Ge, Haibo
supporting information; experimental part, p. 2445 - 2449 (2010/12/25)
An unprecedented C-3-alkenylation of quinolones was reported through palladium-catalyzed C-H functionalization with 1% catalyst loading. This method provides an efficient route to a variety of new quinolone derivatives.
Regioselective synthesis of quinolin-4-ones by pyrolysis of anilinomethylene derivatives of Meldrum's acid
Hill, Lawrence,Imam, S. Haider,McNab, Hamish,O'Neill, William J.
experimental part, p. 1847 - 1851 (2009/12/05)
Electron-rich and electron-deficient anilinomethylene derivatives of Meldrum's acid cyclize equally efficiently to quinolin-4-ones via imidoylketene intermediates under flash vacuum pyrolysis (FVP) conditions. Georg Thieme Verlag Stuttgart.
Gas-phase pyrolysis in organic synthesis: Rapid green synthesis of 4-quinolinones
Al-Awadi, Nouria A.,Abdelhamid, Ismail Abdelshafy,Al-Etaibi, Alya M.,Elnagdi, Mohamed Hilmy
, p. 2205 - 2208 (2008/02/10)
Gas-phase pyrolysis of aminomethylene Meldrum's acid derivatives gave quinolinones and/or amines depending on the nature of arylamino moiety. Effect of substituent on reaction rate and nature of pyrolysis products supports the suggested intramolecular nucleophilic substitution reaction via initially formed keteneamine intermediate. Georg Thieme Verlag Stuttgart.
Exotic amino acids. 8. Synthesis of monomethyl esters of N-aryl-aminomethylenemalonic acids
Zicane,Ravina,Tetere,Rijkure,Petrova,Kalejs
, p. 840 - 845 (2007/10/03)
N-Arylaminomethyleneisopropylidenemalonates, obtained from ethoxymethyleneisopropylidenemalonate and aromatic amines, underwent methanolysis to form monomethyl esters of N-arylaminomethylenemalonic acids. The conditions of their formation and their yields depend on the nature and positions of the substituents in the aromatic ring of the initial amine.
