Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors

Hwan Mook Kim, Kiho Lee, Bum Woo Park, Dong Kyu Ryu, Kangjeon Kim, Chang Woo Lee, Song Kyu Park, Jung Whan Han, Hee Yoon Lee, Hyun Yong Lee, Gyoonhee Han

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26 Citations (Scopus)

Abstract

δ-Lactam-based hydroxamic acids, inhibitors of histone deacetylase (HDAC), have been synthesized via ring closure metathesis of key diene intermediates followed by conversion to hydroxamic acid analogues. The hydroxamic acids 12a, 12b, and 17c showed potent inhibitory activity in HDAC enzyme assay. The hydroxamic acid 12b exhibited growth inhibitory activity on five human tumor cell lines, showing good sensitivity on the MDA-MB-231 breast tumor cell.

Original languageEnglish
Pages (from-to)4068-4070
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number15
DOIs
Publication statusPublished - 2006 Aug 1

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All Science Journal Classification (ASJC) codes

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

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