Artículo
Synthesis and biological evaluation of sphingosine kinase 2 inhibitors with anti‐inflammatory activity
Vettorazzi, Marcela Cristina
; Vila, Laura; Lima, Santiago; Acosta, Lina; Yépes, Felipe; Palma, Alirio; Cobo, Justo; Tengler, Jan; Malik, Ivan; Alvarez, Sergio Eduardo
; Marqués, Patrice; Cabedo, Nuria; Sanz, María J.; Jampilek, Josef; Spiegel, Sarah; Enriz, Ricardo Daniel
Fecha de publicación:
03/2019
Editorial:
Wiley VCH Verlag
Revista:
Archiv Der Pharmazie
ISSN:
0365-6233
e-ISSN:
1521-4184
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
The synthesis of inhibitors of SphK2 with novel structural scaffolds is reported. These compounds were designed from a molecular modeling study, in which the molecular interactions stabilizing the different complexes were taken into account. Particularly interesting is that 7‐bromo‐2‐(2‐phenylethyl)‐2,3,4,5‐tetrahydro‐1,4‐epoxynaphtho[1,2‐b]azepine, which is a selective inhibitor of SphK2, does not exert any cytotoxic effects and has a potent anti‐inflammatory effect. It was found to inhibit mononuclear cell adhesion to the dysfunctional endothelium with minimal impact on neutrophil–endothelial cell interactions. The information obtained from our theoretical and experimental study can be useful in the search for inhibitors of SphK2 that play a prominent role in different diseases, especially in inflammatory and cardiovascular disorders.
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Articulos(IMIBIO-SL)
Articulos de INST. MULTIDICIPLINARIO DE INV. BIO. DE SAN LUIS
Articulos de INST. MULTIDICIPLINARIO DE INV. BIO. DE SAN LUIS
Citación
Vettorazzi, Marcela Cristina; Vila, Laura; Lima, Santiago; Acosta, Lina; Yépes, Felipe; et al.; Synthesis and biological evaluation of sphingosine kinase 2 inhibitors with anti‐inflammatory activity; Wiley VCH Verlag; Archiv Der Pharmazie; 352; 3; 3-2019; 1-14; 1800298
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