Por favor, use este identificador para citar o enlazar este ítem: http://hdl.handle.net/10637/13381
Título : Design and Synthesis ofWater-Soluble and Potent MMP-13 Inhibitors with Activity in Human Osteosarcoma Cells.
Autor : Zapico Rodríguez, José María.
Acosta, Lourdes.
Pastor, Miryam.
Rangasamy, Loganathan.
Márquez-Cantudo, Laura.
Coderch, Claire.
Ortín, Irene.
Nicolau-Sanus, María.
Puchades-Carrasco, Leonor.
Pineda-Lucena, Antonio.
Majali-Martinez, Alejandro.
Ramos Álvarez, Pilar.
Pascual-Teresa Fernández, Beatriz de.
Ramos González, Ana.
Materias: Síntesis orgánica.MMP-13 inhibitorsMetalloproteinasesMolecular modelingOsteoarthritisRMNOrganic synthesis
Fecha de publicación : 15-feb-2021
Resumen : Osteoarthritis is a degenerative disease, often resulting in chronic joint pain and commonly affecting elderly people. Current treatments with anti-inflammatory drugs are palliative, making the discovery of new treatments necessary. The inhibition of matrix metalloproteinase MMP-13 is a validated strategy to prevent the progression of this common joint disorder. We recently described polybrominated benzotriazole derivatives with nanomolar inhibitory activity and a promising selectivity profile against this collagenase. In this work, we have extended the study in order to explore the influence of bromine atoms and the nature of the S10 heterocyclic interacting moiety on the solubility/selectivity balance of this type of compound. Drug target interactions have been assessed through a combination of molecular modeling studies and NMR experiments. Compound 9a has been identified as a water-soluble and highly potent inhibitor with activity in MG-63 human osteosarcoma cells.
Descripción : International Journal Molecular Sciences, e-ISSN 1422-0067, 2021, 22, 9976
Idioma: en
URI : http://hdl.handle.net/10637/13381
Derechos: http://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
Otros identificadores : 000000726403
Aparece en las colecciones: Facultad de Farmacia

Ficheros en este ítem:
Fichero Descripción Tamaño Formato  
Design_Zapico_et_al_Int_J_Mol_Scien_2021.pdf8,6 MBAdobe PDFVisualizar/Abrir

Los ítems de DSpace están protegidos por copyright, con todos los derechos reservados, a menos que se indique lo contrario.