A minimally-masked inactive prodrug of panobinostat that is bioorthogonally activated by gold chemistry

Belén Rubio-ruiz, Ana M. Pérez-lópez, Víctor Sebastián, Asier Unciti-broceta

Research output: Contribution to journalArticlepeer-review

Abstract

The recent incorporation of Au chemistry in the bioorthogonal toolbox has opened up new opportunities to deliver biologically independent reactions in living environments. Herein we report that the O-propargylation of the hydroxamate group of the potent HDAC inhibitor panobinostat leads to a vast reduction of its anticancer properties (>500-fold). We also show that this novel prodrug is converted back into panobinostat in the presence of Au catalysts in vitro and in cell culture
Original languageEnglish
Pages (from-to)116217
JournalBioorganic and Medicinal Chemistry
Early online date15 May 2021
DOIs
Publication statusE-pub ahead of print - 15 May 2021

Keywords

  • Bioorthogonal catalysis
  • gold nanoparticles
  • HDAC inhibitors
  • anticancer therapies

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