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Bioorg Med Chem Lett. 2007 Sep 1;17(17):4895-900. Epub 2007 Jun 13.

Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.

Author information

1
Institute of Molecular and Cellular Biosciences, The University of Tokyo, Yayoi, Tokyo, Japan.

Abstract

We designed and synthesized hydroxamic acid derivatives bearing a 4-(3-pyridyl)phenyl group as a cap structure, and found that they exhibit potent histone deacetylase (HDAC) inhibitory activity. A representative compound, 17a, showed more potent growth-inhibitory activity against pancreatic cancer cells and greater upregulation of p21(WAF1/CIP1) expression than the clinically used HDAC inhibitor suberoylanilide hydroxamic acid (Zolinza).

PMID:
17588744
DOI:
10.1016/j.bmcl.2007.06.038
[Indexed for MEDLINE]

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