Modification of cap group in δ-lactam-based histone deacetylase (HDAC) inhibitors

Hwan Mook Kim, Sung Hee Hong, Myung Sook Kim, Chang Woo Lee, Jong Soon Kang, Kiho Lee, Song Kyu Park, Jeung Whan Han, Hee Yoon Lee, Yongseok Choi, Ho Jeung Kwon, Gyoonhee Han

Research output: Contribution to journalArticlepeer-review

26 Citations (Scopus)


Novel δ-lactam-based HDAC inhibitors which have various substituted benzyl, bi-aromatic cap groups were prepared using ring closure metathesis reaction, and evaluated their HDAC inhibitory activities and anti-proliferative effects. Among prepared analogues, 11m and 11o have very strong HDAC enzymatic inhibition and showed the most potent growth inhibitory activity to five human tumor cell lines including PC-3, ACHN, NUGC-3, HCT-15, and MBA-MB-231 tumor cell lines. Compounds 11m and 11o also showed good tumor growth inhibition of MDA-MB-231 cells in in vivo xenograft model. Structure-activity relationship study using docking model explained the significance of hydrophobic aromatic cap groups for their in vitro activities.

Original languageEnglish
Pages (from-to)6234-6238
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number22
Publication statusPublished - 2007 Nov 15

Bibliographical note

Funding Information:
This research was partly supported by a grant from KRIBB Research Initiative program, a Grant (0405-NS01-0704-0001) of the Korean Health 21 R&D Project, Ministry of Health and Welfare, and the Brain Korea 21 project the Republic of Korea.


  • Anticancer chemotherapy
  • Docking model
  • Enzyme inhibitor
  • Growth inhibition
  • HDAC
  • Histone deacetylase
  • In vivo xenograft model

ASJC Scopus subject areas

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


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