Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 41, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2021.116217
Keywords
Bioorthogonal catalysis; Gold nanoparticles; HDAC inhibitors; Anticancer therapies
Funding
- EPSRC [EP/N021134/1, EP/S010289/1]
- EC [H2020-MSCA-IF-2014-658833]
- Ministerio de Ciencia, Innovacion y Universidades [RTI2018-099019-A-I00]
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The recent incorporation of Au chemistry in bioorthogonal tools has provided new opportunities for delivering biologically independent reactions in living environments. The O-propargylation of the hydroxamate group of panobinostat shows a significant reduction in its anticancer properties, which can be converted back in the presence of Au catalysts.
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.
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