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

Shoukou Lee, Chihiro Shinji, Kiyoshi Ogura, Motomu Shimizu, Satoko Maeda, Mayumi Sato, Minoru Yoshida, Yuichi Hashimoto, Hiroyuki Miyachi

Research output: Contribution to journalArticlepeer-review

42 Citations (Scopus)

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 p21WAF1/CIP1 expression than the clinically used HDAC inhibitor suberoylanilide hydroxamic acid (Zolinza™).

Original languageEnglish
Pages (from-to)4895-4900
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number17
DOIs
Publication statusPublished - Sep 1 2007

Keywords

  • HDAC
  • HDAC inhibitor
  • Hydroxamic acid
  • Isoindoklinone
  • Pancreatic cancer
  • p21

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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