2. Academic Validation
  3. 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

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

  • J Med Chem. 2008 Aug 14;51(15):4370-3. doi: 10.1021/jm8002894.
Alan P Kozikowski 1,  Subhasish Tapadar,  Doris N Luchini,  Ki Hwan Kim,  Daniel D Billadeau
Affiliations

Affiliation

  • 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
PMID: 18642892 DOI: 10.1021/jm8002894
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-18613
    ≥98.0%, HDAC抑制剂
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