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

AuthorsMarco, J. Alberto; García-Plab, Jorge; Carda, Miguel; Murga, Juan; Falomir, Eva; Trigili, Chiara CSIC; Notararigo, Sara CSIC; Díaz, José Fernando CSIC ORCID ; Barasoain, Isabel CSIC ORCID
Tubulin-active compound
Microtubule destabilization
Pironetin analogue
Issue DateMay-2011
CitationEuropean Journal of Medicinal Chemistry 46(5):1630-1637(2011)
AbstractThe 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
Description8 páginas, 4 figuras, 1 tabla, 2 esquemas -- PAGS nros. 1630-1637
Publisher version (URL)http://dx.doi.org/10.1016/j.ejmech.2011.02.011
Appears in Collections:(CIB) Artículos
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