716-11-0Relevant articles and documents
COMPOUNDS TARGETING DUAL G-QUADRUPLEX DNA AND STAT3
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Page/Page column 31; 36-38, (2021/01/23)
The present invention relates to novel quinazoline compounds having the formula (I) or (II): (I) (II). The compounds are active both as stabilizers of G-quadruplex DNA structures and as inhibitors of STAT3 phosphorylation. The disclosed compounds are useful in medical treatment, such as the treatment of cancer.
Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure
Soubhye, Jalal,Chikh Alard, Ibaa,Aldib, Iyas,Prévost, Martine,Gelbcke, Michel,De Carvalho, Annelise,Furtmüller, Paul G.,Obinger, Christian,Flemmig, J?rg,Tadrent, Sara,Meyer, Franck,Rousseau, Alexandre,Nève, Jean,Mathieu, Véronique,Zouaoui Boudjeltia, Karim,Dufrasne, Fran?ois,Van Antwerpen, Pierre
, p. 6563 - 6586 (2017/08/17)
The heme enzyme myeloperoxidase (MPO) participates in innate immune defense mechanism through formation of microbicidal reactive oxidants. However, evidence has emerged that MPO-derived oxidants contribute to propagation of inflammatory diseases. Because of the deleterious effects of circulating MPO, there is a great interest in the development of new efficient and specific inhibitors. Here, we have performed a novel virtual screening procedure, depending on ligand-based pharmacophore modeling followed by structure-based virtual screening. Starting from a set of 727842 compounds, 28 molecules were selected by this virtual method and tested on MPO in vitro. Twelve out of 28 compounds were found to have an IC50 less than 5 μM. The best inhibitors were 2-(7-methoxy-4-methylquinazolin-2-yl)guanidine (28) and (R)-2-(1-((2,3-dihydro-1H-imidazol-2-yl)methyl)pyrrolidin-3-yl)-5-fluoro-1H-benzo[d]imidazole (42) with IC50 values of 44 and 50 nM, respectively. Studies on the mechanism of inhibition suggest that 28 is the first potent mechanism-based inhibitor and inhibits irreversibly MPO at nanomolar concentration.
Compounds for the treatment of pain
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, (2008/06/13)
This invention provides methods of treating pain, urinary incontinence and other abnormalities mediated by a NPFF receptor, which comprises administering to a subject a therapeutically effective amount of a chemical compound which acts at the NPFF1 receptor, the NPFF2 receptor, or at both the NPFF1 and NPFF2 receptors.