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J Med Chem. 2008 Aug 14;51(15):4370-3. doi: 10.1021/jm8002894. Epub 2008 Jul 22.

Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.

Author information

1
Department of Medicinal Chemistry & Pharmacognosy, Drug Discovery Program, University of Illinois at Chicago, 833 South Wood Street, Chicago, Illinois 60612, USA. Kozikowa@uic.edu

Abstract

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 approximately 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.

PMID:
18642892
PMCID:
PMC3913184
DOI:
10.1021/jm8002894
[Indexed for MEDLINE]
Free PMC Article

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