Structure−Activity Relationship Studies of a Series of Novel δ-Lactam-Based Histone Deacetylase Inhibitors

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...

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Veröffentlicht in:Journal of medicinal chemistry 2007-05, Vol.50 (11), p.2737-2741
Hauptverfasser: Kim, Hwan Mook, Ryu, Dong-Kyu, Choi, Yongseok, Park, Bum Woo, Lee, Kiho, Han, Sang Bae, Lee, Chang-Woo, Kang, Moo-Rim, Kang, Jong Soon, Boovanahalli, Shanthaveerappa K, Park, Song-Kyu, Han, Jung Whan, Chun, Tae-Gyu, Lee, Hee-Yoon, Nam, Ky-Youb, Choi, Eun Hyun, Han, Gyoonhee
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Sprache:eng
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Zusammenfassung: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 anti-inflammatory 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
1520-4804
DOI:10.1021/jm0613828