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

Daniele Passarella, Daniela Comi, Andrea Vanossi, Gianfranco Paganini, Francesco Colombo, Luca Ferrante, Valentina Zuco, Bruno Danieli, Franco Zunino

Research output: Contribution to journalArticle

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.

Original languageEnglish
Pages (from-to)6358-6363
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number22
DOIs
Publication statusPublished - 2009

Keywords

  • Anticancer compounds
  • Disulfide bond
  • HDAC inhibitors
  • Releasable conjugate compounds
  • Tubulin binders

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Fingerprint Dive into the research topics of 'Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds'. Together they form a unique fingerprint.

  • Cite this

    Passarella, D., Comi, D., Vanossi, A., Paganini, G., Colombo, F., Ferrante, L., Zuco, V., Danieli, B., & Zunino, F. (2009). Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds. Bioorganic and Medicinal Chemistry Letters, 19(22), 6358-6363. https://doi.org/10.1016/j.bmcl.2009.09.075