Structure-activity relationship studies of a series of novel δ-lactam-based histone deacetylase inhibitors

Mook Kim Hwan, Dong Kyu Ryu, Yongseok Choi, Woo Park Bum, Kiho Lee, Bae Han Sang, Chang Woo Lee, Moo Rim Kang, Soon Kang Jong, Shanthaveerappa K. Boovanahalli, Song Kyu Park, Whan Han Jung, Tae Gyu Chun, Hee Yoon Lee, Ky Youb Nam, Hyun Choi Eun, Gyoonhee Han

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Abstract

We synthesized a series of δ-lactam-based HDAC inhibitors that were identified with various degrees of anti-inflammatory and cell growth inhibitory activities. Compounds possessing significant HDAC inhibitory activity exhibited both anti-inflammatory and cell growth inhibitory activities as well as significant tumor growth inhibition in the in vivo tumor xenograft experiments. Besides, these compounds demonstrated antiinflammatory properties in vitro via suppression of the production of the proinflammatory cytokine TNF-α and nitric oxide by LPS-stimulated RAW264.7 cells.

Original languageEnglish
Pages (from-to)2737-2741
Number of pages5
JournalJournal of Medicinal Chemistry
Volume50
Issue number11
DOIs
Publication statusPublished - 2007 May 31

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All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

Cite this

Hwan, M. K., Ryu, D. K., Choi, Y., Bum, W. P., Lee, K., Sang, B. H., Lee, C. W., Kang, M. R., Jong, S. K., Boovanahalli, S. K., Park, S. K., Jung, W. H., Chun, T. G., Lee, H. Y., Nam, K. Y., Eun, H. C., & Han, G. (2007). Structure-activity relationship studies of a series of novel δ-lactam-based histone deacetylase inhibitors. Journal of Medicinal Chemistry, 50(11), 2737-2741. https://doi.org/10.1021/jm0613828