1‐Arylsulfonyl‐5‐(N‐hydroxyacrylamide)indolines Histone Deacetylase Inhibitors Are Potent Cytokine Release Suppressors. Issue 10 (20th June 2013)

• Record Type: Journal Article
• Authors: Lee, Hsueh‐Yun; Yang, Chia‐Ron; Lai, Mei‐Jung; Huang, Han‐Li; Hsieh, Yi‐Ling; Liu, Yi‐Min; Yeh, Teng‐Kuang; Li, Yu‐Hsuan; Mehndiratta, Samir; Teng, Che‐Ming; Liou, Jing‐Ping
• Is Part Of: Chembiochem. Volume 14:Issue 10(2013)
• Page Start: 1248
• Page End: 1254
• Publication Date: 2013-06-20
• Subjects: Biochemistry -- Periodicals; Molecular biology -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1002/cbic.201300201
• Languages: English
• ISSNs: 1439-4227

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>A series of 1‐arylsulfonyl‐5‐(<italic>N</italic>‐hydroxyacrylamide)indolines (<bold>7</bold>–<bold>15</bold>) has been developed; the compounds exhibited potent histone deacetylase (HDAC) inhibitory activities. Notably, almost all of this series exhibited better HDAC‐inhibitory and antiproliferative activities than 3‐(1‐benzenesulfonyl‐1<italic>H</italic>‐indol‐5‐yl)‐<italic>N</italic>‐hydroxyacrylamide (<bold>6</bold>), as reported in a previous study. Among these compounds, 3‐[1‐(4‐methoxybenzenesulfonyl)‐2, 3‐dihydro‐1<italic>H</italic>‐indol‐5‐yl]‐<italic>N</italic>‐hydroxyacrylamide (<bold>9</bold>) showed a two‐ to tenfold increase in activity compared to SAHA (<bold>1</bold>) in the suppression of lipopolysaccharide‐induced cytokine production. Compound <bold>9</bold> also caused a marked reduction in carrageenan‐induced acute inflammation in a rat model. Taken together, these data indicated that 1‐arylsulfonyl‐5‐(<italic>N</italic>‐hydroxyacrylamide)indolines HDAC inhibitors exhibit potent anti‐inflammatory activity.</p> </abstract>