Design and synthesis of phthalimide-type histone deacetylase inhibitors

Chihiro Shinji, Takanori Nakamura, Satoko Maeda, Minoru Yoshida, Yuichi Hashimoto, Hiroyuki Miyachi

Research output: Contribution to journalArticlepeer-review

51 Citations (Scopus)


Several hydroxamic acid derivatives with a substituted phthalimide group as a linker and/or cap structure, prepared during structural development studies based on thalidomide, were found to have histone deacetylase (HDAC)-inhibitory activity. Structure-activity relationship studies indicated that nature of the substituent introduced at the phthalimide nitrogen atom, introduction of a hydroxamic acid structure, and distance between the N-hydroxyl group and the cap structure are important for HDAC-inhibitory activity.

Original languageEnglish
Pages (from-to)4427-4431
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number20
Publication statusPublished - Oct 15 2005


  • HDAC inhibitor
  • Phthalimide
  • Thalidomide

ASJC Scopus subject areas

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


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