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

Authors:Marco, J. Alberto
García-Plab, Jorge
Carda, Miguel
Murga, Juan
Falomir, Eva
Trigili, Chiara
Notararigo, Sara
Díaz, José Fernando
Barasoain, Isabel
Keywords:Tubulin, Tubulin-active compound, Microtubule destabilization, Pironetin analogue, Cytotoxicity
Issue Date:May-2011
Publisher:Elsevier
Citation:European Journal of Medicinal Chemistry 46(5):1630-1637(2011)
Abstract:The 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
Description:8 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
URI:http://hdl.handle.net/10261/51844
ISSN:0223-5234
E-ISSNmetadata.dc.identifier.doi = DOI:1768-3254
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