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http://hdl.handle.net/10261/216740
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dc.contributor.author | Arévalo-Ruiz, Matilde | - |
dc.contributor.author | Amrane, S. | - |
dc.contributor.author | Rosu, F. | - |
dc.contributor.author | Belmonte-Reche, Efres | - |
dc.contributor.author | Peñalver, Pablo | - |
dc.contributor.author | Mergny, Jean-Louis | - |
dc.contributor.author | Morales, Juan C. | - |
dc.date.accessioned | 2020-07-16T09:20:18Z | - |
dc.date.available | 2020-07-16T09:20:18Z | - |
dc.date.issued | 2020 | - |
dc.identifier | doi: 10.1016/j.bioorg.2020.103786 | - |
dc.identifier | issn: 0045-2068 | - |
dc.identifier | e-issn: 1090-2120 | - |
dc.identifier.citation | Bioorganic Chemistry 99 (2020) | - |
dc.identifier.uri | http://hdl.handle.net/10261/216740 | - |
dc.description.abstract | Here we present a novel G4-binding family of compounds based on a central core of phenyl ditriazole (PDTZ) modified with carbohydrates and phenyl pyrrolidinyl side-chains. Their synthesis was achieved using controlled click chemistry conditions to obtain both, symmetric and dissymmetric carb-PDTZ derivatives without any intermediate protecting steps through an optimized methodology. Binding of the new carb-PDTZ to a variety of G-quadruplex motifs was examined using different biophysical techniques. The symmetric carb-PDTZ derivatives were not able to stabilize G4, but the dissymmetric ones (containing one sugar and one phenyl pyrrolidinyl side-chain) did. Interestingly, the dissymmetric carb-PDTZ derivatives showed much higher G4 vs duplex DNA selectivity than the control compound PDTZ 1, which contains two phenyl pyrrodilinyl side-chains and no carbohydrates. Their potential antitumoral activity was also investigated by in vitro cytotoxicity measurements on different cancerous cell lines. All carb-PDTZ derivatives showed higher IC values than the control PDTZ 1, probably due to the lack of compound stability of some derivatives and to lower cellular uptake. | - |
dc.language | eng | - |
dc.publisher | Elsevier | - |
dc.rights | closedAccess | - |
dc.subject | DNA | - |
dc.subject | G-quadruplex | - |
dc.subject | Ligand | - |
dc.subject | Conjugates | - |
dc.subject | Carbohydrates | - |
dc.title | Symmetric and dissymmetric carbohydrate-phenyl ditriazole derivatives as DNA G-quadruplex ligands: Synthesis, biophysical studies and antiproliferative activity | - |
dc.type | artículo | - |
dc.identifier.doi | 10.1016/j.bioorg.2020.103786 | - |
dc.relation.publisherversion | http://dx.doi.org/10.1016/j.bioorg.2020.103786 | - |
dc.date.updated | 2020-07-16T09:20:19Z | - |
dc.relation.csic | Sí | - |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.fulltext | No Fulltext | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.cerifentitytype | Publications | - |
item.grantfulltext | none | - |
item.openairetype | artículo | - |
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