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

Research output: Contribution to journalArticle

29 Citations (Scopus)

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

Fingerprint

Lactams
Histone Deacetylase Inhibitors
Structure-Activity Relationship
Anti-Inflammatory Agents
Growth
Heterografts
Neoplasms
Nitric Oxide
Cytokines

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

Cite this

Hwan, Mook Kim ; Ryu, Dong Kyu ; Choi, Yongseok ; Bum, Woo Park ; Lee, Kiho ; Sang, Bae Han ; Lee, Chang Woo ; Kang, Moo Rim ; Jong, Soon Kang ; Boovanahalli, Shanthaveerappa K. ; Park, Song Kyu ; Jung, Whan Han ; Chun, Tae Gyu ; Lee, Hee Yoon ; Nam, Ky Youb ; Eun, Hyun Choi ; Han, Gyoonhee. / Structure-activity relationship studies of a series of novel δ-lactam-based histone deacetylase inhibitors. In: Journal of Medicinal Chemistry. 2007 ; Vol. 50, No. 11. pp. 2737-2741.
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Hwan, MK, Ryu, DK, Choi, Y, Bum, WP, Lee, K, Sang, BH, Lee, CW, Kang, MR, Jong, SK, Boovanahalli, SK, Park, SK, Jung, WH, Chun, TG, Lee, HY, Nam, KY, Eun, HC & Han, G 2007, 'Structure-activity relationship studies of a series of novel δ-lactam-based histone deacetylase inhibitors', Journal of Medicinal Chemistry, vol. 50, no. 11, pp. 2737-2741. https://doi.org/10.1021/jm0613828

Structure-activity relationship studies of a series of novel δ-lactam-based histone deacetylase inhibitors. / Hwan, Mook Kim; Ryu, Dong Kyu; Choi, Yongseok; Bum, Woo Park; Lee, Kiho; Sang, Bae Han; Lee, Chang Woo; Kang, Moo Rim; Jong, Soon Kang; Boovanahalli, Shanthaveerappa K.; Park, Song Kyu; Jung, Whan Han; Chun, Tae Gyu; Lee, Hee Yoon; Nam, Ky Youb; Eun, Hyun Choi; Han, Gyoonhee.

In: Journal of Medicinal Chemistry, Vol. 50, No. 11, 31.05.2007, p. 2737-2741.

Research output: Contribution to journalArticle

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AU - Hwan, Mook Kim

AU - Ryu, Dong Kyu

AU - Choi, Yongseok

AU - Bum, Woo Park

AU - Lee, Kiho

AU - Sang, Bae Han

AU - Lee, Chang Woo

AU - Kang, Moo Rim

AU - Jong, Soon Kang

AU - Boovanahalli, Shanthaveerappa K.

AU - Park, Song Kyu

AU - Jung, Whan Han

AU - Chun, Tae Gyu

AU - Lee, Hee Yoon

AU - Nam, Ky Youb

AU - Eun, Hyun Choi

AU - Han, Gyoonhee

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