Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: Effects on HDAC biology and antiproliferative activity

Subhasish Tapadar, Rong He, Doris N. Luchini, Daniel D. Billadeau, Alan P. Kozikowski

Research output: Contribution to journalArticle

28 Scopus citations

Abstract

A series of hydroxamic acid based histone deacetylase inhibitors 6-15, containing an isoxazole moiety adjacent to the Zn-chelating hydroxamic acid, is reported herein. Some of these compounds showed nanomolar activity in the HDAC isoform inhibitory assay and exhibited micro molar inhibitory activity against five pancreatic cancer cell lines.

Original languageEnglish (US)
Pages (from-to)3023-3026
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number11
DOIs
StatePublished - Jun 1 2009

Keywords

  • HDAC
  • HDAC inhibitor
  • Isoform
  • Pancreatic cancer

ASJC Scopus subject areas

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

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