Synthesis of new β-lactam analogs and evaluation of their histone deacetylase (HDAC) activity

Seikwan Oh, Jae Chul Jung

Research output: Contribution to journalArticlepeer-review

13 Scopus citations


A simple synthesis of the β-lactams 11-13 and 16-17 as novel histone deacetylase (HDAC) inhibitors is described. The key synthetic strategies involved the O-alkylation of 6-APA and the coupling reactions of freshly prepared N-carbobenzyloxy-L-prolines 5 and 6 and 6-aminopenicillanates 8-10 and 15 in high yields. It was found that all compounds show potent growth inhibitory activity on human tumor cell lines, the most potent compound 16 exhibiting an IC50 = 2.1 μM in vitro.

Original languageEnglish
Pages (from-to)1459-1464
Number of pages6
JournalZeitschrift fur Naturforschung - Section B Journal of Chemical Sciences
Issue number11
StatePublished - Nov 2007

Bibliographical note

Funding Information:
This work has been supported by the KOSEF Brain Neurobiology Grant (2007), by the Ewha Global Challenge (BK21) grant, and in part by Cooperative Agreement Number 1-U01 C1000211 from the Centers for Disease Control and Prevention (M. A. A.).


  • Anticancer
  • Coupling reaction
  • Histone deacetylase
  • Synthesis
  • β-lactams


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