20780-75-0Relevant academic research and scientific papers
Inhibitor of the human telomerase reverse trancriptase (hTERT) gene promoter induces cell apoptosis via a mitochondrial-dependent pathway
Li, Yuyin,Pan, Guojun,Chen, Yue,Yang, Qian,Hao, Tiantian,Zhao, Lianbo,Zhao, Long,Cong, Yusheng,Diao, Aipo,Yu, Peng
, p. 370 - 378 (2018/01/17)
Telomerase is aberrantly expressed in many cancers and plays an important role in the development of cellular immortality and oncogenesis, which makes it a potential cancer therapeutic target for drug discovery. Here, we constructed a firefly luciferase r
NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS
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Page/Page column 40, (2018/01/19)
Provided are certain pyrazine derivatives (I) as SHP2 inhibitors which is shown as formula (I), their synthesis and their use for treating a SHP2 mediated disorder. More particularly, provided are fused heterocyclic derivatives useful as inhibitors of SHP
Counter-current chromatography separation of isatin derivatives using the sandmeyer methodology
Almeida, Ma?rcia R.,Leita?o, Gilda G.,Silva, Ba?rbara V.,Barbosa, Jussara P.,Pintoa, Angelo C.
scheme or table, p. 764 - 769 (2010/08/13)
A rapid and efficient method, using high-speed counter-current chromatography (HSCCC) technique, was developed for the separation of isomeric isatin derivatives, prepared following the Sandmeyer route. The biphasic solvent system composed of hexane:ethyl acetate:ethanol:water 1:0.5:0.5:1 (v/v/v/v) was used for all separations.
Direct synthesis of new arylanthranilic acids via a Suzuki cross-coupling reaction from iodoisatins
Gérard, Anne-Laure,Lisowski, Vincent,Rault, Sylvain
, p. 6082 - 6087 (2007/10/03)
Direct synthesis of new arylanthranilic acids via a Suzuki cross-coupling reaction with iodoisatins as key intermediates is described. A 'one pot' procedure is proposed.
INDIRUBIN-TYPE COMPOUNDS, COMPOSITIONS, AND METHODS FOR THEIR USE
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Page/Page column 24; Figure 2A, (2008/06/13)
Compounds and compositions including 6-bromo-indirubin, 5-amino-indirubin and N-methyl-indirubins and related indirubin derivatives are provided that are useful as selective modulators of glycogen synthase kinase-3, cyclin-dependent protein kinases or aryl hydrocarbon receptors. Methods of inhibiting or modulating cell growth or cell cycling are provided using the compounds of the invention. In other aspects, compounds and methods for the treatment of protozoan-mediated diseases, Alzheimer's disease and diabetes are provided.
Structural Basis for the Synthesis of Indirubins as Potent and Selective Inhibitors of Glycogen Synthase Kinase-3 and Cyclin-Dependent Kinases
Polychronopoulos, Panagiotis,Magiatis, Prokopios,Skaltsounis, Alexios-Leandros,Myrianthopoulos, Vassilios,Mikros, Emmanuel,Tarricone, Aldo,Musacchio, Andrea,Roe, S. Mark,Pearl, Laurence,Leost, Maryse,Greengard, Paul,Meijer, Laurent
, p. 935 - 946 (2007/10/03)
Pharmacological inhibitors of glycogen synthase kinase-3 (GSK-3) and cyclin-dependent kinases have a promising potential for applications against several neurodegenerative diseases such as Alzheimer's disease. Indirubins, a family of bis-indoles isolated from various natural sources, are potent inhibitors of several kinases, including GSK-3. Using the cocrystal structures of various indirubins with GSK-3β, CDK2 and CDK5/p25, we have modeled the binding of indirubins within the ATP-binding pocket of these kinases. This modeling approach provided some insight into the molecular basis of indirubins' action and selectivity and allowed us to forecast some improvements of this family of bis-indoles as kinase inhibitors. Predicted molecules, including 6-substituted and 5,6-disubstituted indirubins, were synthesized and evaluated as CDK and GSK-3 inhibitors. Control, kinase-inactive indirubins were obtained by introduction of a methyl substitution on N1.
Pyridazinedione compounds useful in treating neurological disorders
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, (2008/06/13)
The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.
Synthesis of iodine-123 labelled analogues of the partial agonist (S)- and (R)-bretazenil for the study of CNS benzodiazepine receptors using SPECT
Katsifis, Andrew,Mattner, Filomena,McPhee, Meredith,Kassiou, Michael,Najdovski, Ljubco,Dikic, Branko
, p. 835 - 845 (2007/10/03)
The (S) and (R)-[123I]iodinated analogues of the benzodiazepine receptor partial agonist bretazenil have been synthesised for study of the central benzodiazepine receptor using SPECT. (S)- and (R)-[123I]iodobretazenil were prepared from the appropriate tin precursors by electrophilic iododestannylation with Na[123I] in the presence of Chloramine-T. The products were purified by semi-preparative reverse-phase HPLC with radiochemical yields of 80% in a total synthesis time of 50 minutes. The specific activity was determined to be greater than 2500 Ci/mmol. The radiochemical and chemical purity assessed by radio-TLC and HPLC were found to be 98%. The enantiomeric purity of the (S) and (R) isomers were greater than 97% as assessed by analytical chiral HPLC analysis.
