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

doi:10.1021/jm0613828

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 journal › Article › peer-review

31 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 language	English
Pages (from-to)	2737-2741
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	50
Issue number	11
DOIs	https://doi.org/10.1021/jm0613828
Publication status	Published - 2007 May 31

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

Access to Document

10.1021/jm0613828

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

@article{d97816423a3545cdb91495596f7a0359,

title = "Structure-activity relationship studies of a series of novel δ-lactam-based histone deacetylase inhibitors",

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.",

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

year = "2007",

month = may,

day = "31",

doi = "10.1021/jm0613828",

language = "English",

volume = "50",

pages = "2737--2741",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "11",

}

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

TY - JOUR

T1 - Structure-activity relationship studies of a series of novel δ-lactam-based histone deacetylase inhibitors

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

PY - 2007/5/31

Y1 - 2007/5/31

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=34250203882&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=34250203882&partnerID=8YFLogxK

U2 - 10.1021/jm0613828

DO - 10.1021/jm0613828

M3 - Article

C2 - 17477518

AN - SCOPUS:34250203882

SN - 0022-2623

VL - 50

SP - 2737

EP - 2741

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 11

ER -

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

Abstract

All Science Journal Classification (ASJC) codes

Access to Document

Other files and links

Fingerprint

Cite this