Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) …
AP Kozikowski, S Tapadar, DN Luchini… - Journal of medicinal …, 2008 - ACS Publications
AP Kozikowski, S Tapadar, DN Luchini, KH Kim, DD Billadeau
Journal of medicinal chemistry, 2008•ACS PublicationsA series of hydroxamate based HDAC inhibitors containing a phenylisoxazole as the CAP
group has been synthesized using nitrile oxide cycloaddition chemistry. An HDAC6 selective
inhibitor having a potency of∼ 2 picomolar was identified. Some of the compounds were
examined for their ability to block pancreatic cancer cell growth and found to be about 10-
fold more potent than SAHA. This research provides valuable, new molecular probes for use
in exploring HDAC biology.
group has been synthesized using nitrile oxide cycloaddition chemistry. An HDAC6 selective
inhibitor having a potency of∼ 2 picomolar was identified. Some of the compounds were
examined for their ability to block pancreatic cancer cell growth and found to be about 10-
fold more potent than SAHA. This research provides valuable, new molecular probes for use
in exploring HDAC biology.
A series of hydroxamate based HDAC inhibitors containing a phenylisoxazole as the CAP group has been synthesized using nitrile oxide cycloaddition chemistry. An HDAC6 selective inhibitor having a potency of ∼2 picomolar was identified. Some of the compounds were examined for their ability to block pancreatic cancer cell growth and found to be about 10-fold more potent than SAHA. This research provides valuable, new molecular probes for use in exploring HDAC biology.
ACS Publications