2. Academic Validation
  3. Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds

Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds

  • Bioorg Med Chem Lett. 2009 Nov 15;19(22):6358-63. doi: 10.1016/j.bmcl.2009.09.075.
Daniele Passarella 1,  Daniela Comi,  Andrea Vanossi,  Gianfranco Paganini,  Francesco Colombo,  Luca Ferrante,  Valentina Zuco,  Bruno Danieli,  Franco Zunino
Affiliations

Affiliation

  • 1 Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, Italy. Daniele.Passarella@unimi.it
PMID: 19833515 DOI: 10.1016/j.bmcl.2009.09.075
Abstract

Design and synthesis of an HDAC Inhibitor and its merger with three tubulin Binders to create releasable conjugate compounds is described. The biological evaluation includes: (a) in vitro reactivity with glutathione, (b) antiproliferative activity, (c) cell cycle analysis and (d) quantification of protein acetylation. The cellular pharmacology study indicated that the HDAC-inhibitor-drug conjugates retained antimitotic and proapoptotic activity with a reduced potency.

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