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Title 

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

Authors 

Hwan Mook KimD K RyuY ChoiBum Woo ParkKiho LeeSang Bae HanChang-Woo LeeMoo-Rim KangJong Soon KangS K BoovanahalliSong Kyu ParkJ W HanT G ChunH Y LeeK Y NamE H ChoiG Han

Publisher 

American Chemical Society

Issue Date 

2007

Citation 

Journal of Medicinal Chemistry, vol. 50, no. 11, pp. 2737-2741

Keywords 

dela lactamhistone deacetylase inhibitorlactam derivativetumor necrosis factor alphaantiinflammatory activityin vitro studyanimalsanti-inflammatory agents, non-steroidalantineoplastic agentsdrug screening assays, antitumor

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.

ISSN 

0022-2623

Link 

http://dx.doi.org/10.1021/jm0613828

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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