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Título

Design and Synthesis of Pironetin Analogues with Simplified Structure and Study of Their Interactions with Microtubules

AutorMarco, J. Alberto; García-Pla, Jorge; Carda, Miguel; Murga, Juan; Falomir, Eva; Trigili, Chiara CSIC; Notararigo, Sara CSIC ORCID; Díaz, José Fernando CSIC ORCID ; Barasoain, Isabel CSIC
Palabras claveTubulin
Tubulin-active compound
Microtubule destabilization
Pironetin analogue
Cytotoxicity
Fecha de publicaciónmay-2011
EditorElsevier
CitaciónEuropean Journal of Medicinal Chemistry 46(5):1630-1637(2011)
ResumenThe preparation of a series of pironetin analogues with simplified structure is described. Their cytotoxic activity and their interactions with tubulin have been investigated. It has been found that, while less active than the parent molecule, the pironetin analogues still share the mechanism of action of the latter and compete for the same binding site to α-tubulin. Variations in the configurations of their stereocenters do not translate into relevant differences between biological activities
Descripción8 páginas, 4 figuras, 1 tabla, 2 esquemas -- PAGS nros. 1630-1637
Versión del editorhttp://dx.doi.org/10.1016/j.ejmech.2011.02.011
URIhttp://hdl.handle.net/10261/51844
DOI10.1016/j.ejmech.2011.02.011
ISSN0223-5234
E-ISSN1768-3254
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