685103-95-1Relevant academic research and scientific papers
Structure-Activity-Relationship-Aided Design and Synthesis of xCT Antiporter Inhibitors
Cirillo, Davide,Sarowar, Shahin,?yvind Enger, Per,Bj?rsvik, Hans-René
, p. 2650 - 2668 (2021/06/01)
The xCT antiporter is a cell membrane protein involved in active counter-transportation of glutamate (outflux) with cystine (influx) over the human cell membrane. This feature makes the xCT antiporter a crucial element of the biosynthesis of the vital free radical scavenger glutathione. The prodrug sulfasalazine, a medication for the treatment of ulcerative colitis, was previously proven to inhibit the xCT antiporter. Starting from sulfasalazine, a molecular scaffold jumping followed by SAR-assisted design and synthesis provided a series of styryl hydroxy-benzoic acid analogues that were biologically tested in vitro for their ability to decrease intracellular glutathione levels using four different cancer cell lines: A172 (glioma), A375 (melanoma), U87 (glioma) and MCF7 (breast carcinoma). Depletion of glutathione levels varied among the compounds as well as among the cell lines. Flow cytometry using propidium iodide and the annexin V marker demonstrated minimal toxicity in normal human astrocytes for a promising candidate molecule (E)-5-(2-([1,1′-biphenyl]-4-yl)vinyl)-2-hydroxybenzoic acid.
Preparation method of substituted piperidine derivative
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Paragraph 0023-0024, (2018/04/02)
The invention discloses a preparation method of a substituted piperidine derivative: 4-((2-(aminomethyl)-4-iodophenoxy)methyl)piperidine-1-tert-butyl formate. 5-iodine-2-hydroxybenzaldehyde is used asa starting raw material, and oximation, elimination, et
2,3-DIHYDROIMIDAZO[1 ,2-c] PYRIMIDIN-5(1 H)-ONE COMPOUNDS USE AS LP-PLA2 INHIBITORS
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Paragraph 0797, (2014/07/08)
Disclosed are 2,3-dihydroimidazo[1,2-c]pyrimidin-5(1H)-one compounds that inhibit Lp-PLA2, processes for their preparation, compositions containing them and their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
BICYCLIC PYRIMIDONE COMPOUNDS
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Paragraph 0184, (2014/07/08)
The present invention relates to novel bicyclic pyrimidone compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
BICYCLIC PYRIMIDONE COMPOUNDS
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Page/Page column 27, (2013/03/26)
The present invention relates to novel bicyclic pyrimidone compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
2,3-DIHYDROIMIDAZO[1,2-C] PYRIMIDIN-5(1H)-ONE COMPOUNDS USE AS LP-PLA2 INHIBITORS
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Page/Page column 83, (2013/03/26)
Disclosed are 2,3-dihydroimidazo[1,2-c]pyrimidin-5(1H)-one compounds that inhibit Lp-PLA2, processes for their preparation, compositions containing them and their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer?s disease
TRICYCLIC COMPOUNDS, PREPARATION METHODS, AND THEIR USES
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Page/Page column 34-35, (2012/04/10)
The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
Concise and modular synthesis of regioisomeric haptens for the production of high-affinity and stereoselective antibodies to the strobilurin azoxystrobin
Parra, Javier,Mercader, Josep V.,Agulló, Consuelo,Abad-Fuentes, Antonio,Abad-Somovilla, Antonio
experimental part, p. 624 - 635 (2011/03/19)
The immune response to regioisomeric haptens of azoxystrobin with varied derivatization sites was studied. Based on the Sonogashira and Suzuki-Miyaura couplings and following a straightforward modular design, we have synthesized four haptens with the same linker anchored through C-C bonds and located at different sites of the molecule. The most stereoselective antibodies were produced from immunogens with the spacer arm at a distal position from the β-methoxyacrylate moiety characteristic of strobilurins. Moreover, we observed that assay cross-reactivity was reliant on the functionalization site of the competitor derivative. Finally, the antibody binding site was explored using synthetic chemical analogues.
