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

Research output: Contribution to journalArticle

25 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

Fingerprint

Hydroxamic Acids
Lactams
Histone Deacetylase Inhibitors
Cell growth
Growth
Tumors
Neoplasms
Cells
Histone Deacetylases
Enzyme Assays
Tumor Cell Line
Assays
Breast Neoplasms
Enzymes

All Science Journal Classification (ASJC) codes

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

Cite this

Kim, Hwan Mook ; Lee, Kiho ; Park, Bum Woo ; Ryu, Dong Kyu ; Kim, Kangjeon ; Lee, Chang Woo ; Park, Song Kyu ; Han, Jung Whan ; Lee, Hee Yoon ; Lee, Hyun Yong ; Han, Gyoonhee. / Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2006 ; Vol. 16, No. 15. pp. 4068-4070.
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Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors. / Kim, Hwan Mook; Lee, Kiho; Park, Bum Woo; Ryu, Dong Kyu; Kim, Kangjeon; Lee, Chang Woo; Park, Song Kyu; Han, Jung Whan; Lee, Hee Yoon; Lee, Hyun Yong; Han, Gyoonhee.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 15, 01.08.2006, p. 4068-4070.

Research output: Contribution to journalArticle

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