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

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

  • Bioorg Med Chem Lett. 2007 Sep 1;17(17):4895-900. doi: 10.1016/j.bmcl.2007.06.038.
Shoukou Lee 1,  Chihiro Shinji,  Kiyoshi Ogura,  Motomu Shimizu,  Satoko Maeda,  Mayumi Sato,  Minoru Yoshida,  Yuichi Hashimoto,  Hiroyuki Miyachi
Affiliations

Affiliation

  • 1 Institute of Molecular and Cellular Biosciences, The University of Tokyo, Yayoi, Tokyo, Japan.
PMID: 17588744 DOI: 10.1016/j.bmcl.2007.06.038
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).

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