2. Academic Validation
  3. Design and synthesis of pironetin analogues with simplified structure and study of their interactions with microtubules

Design and synthesis of pironetin analogues with simplified structure and study of their interactions with microtubules

  • Eur J Med Chem. 2011 May;46(5):1630-7. doi: 10.1016/j.ejmech.2011.02.011.
J Alberto Marco 1,  Jorge García-Pla,  Miguel Carda,  Juan Murga,  Eva Falomir,  Chiara Trigili,  Sara Notararigo,  J Fernando Díaz,  Isabel Barasoain
Affiliations

Affiliation

  • 1 Department de Q. Orgánica, University de Valencia, c/ D. Moliner 50, E-46100 Burjassot, Valencia, Spain. alberto.marc@uv.es
PMID: 21396747 DOI: 10.1016/j.ejmech.2011.02.011
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.

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