Lee H.-Y.CHIA-RON YANGLai M.-J.Huang H.-L.Hsieh Y.-L.Liu Y.-M.Yeh T.-K.Li Y.-H.Mehndiratta S.Teng C.-M.Liou J.-P.2021-06-042021-06-04201314394227https://www.scopus.com/inward/record.uri?eid=2-s2.0-84879840340&doi=10.1002%2fcbic.201300201&partnerID=40&md5=b41a82d325f2bb9049b3ba42f1235042https://scholars.lib.ntu.edu.tw/handle/123456789/565282A series of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indolines (7-15) 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-1H-indol-5-yl)-N-hydroxyacrylamide (6), as reported in a previous study. Among these compounds, 3-[1-(4-methoxybenzenesulfonyl)-2,3-dihydro-1H-indol-5-yl]-N-hydroxyacrylamide (9) showed a two- to tenfold increase in activity compared to SAHA (1) in the suppression of lipopolysaccharide-induced cytokine production. Compound 9 also caused a marked reduction in carrageenan-induced acute inflammation in a rat model. Taken together, these data indicated that 1-arylsulfonyl-5-(N-hydroxyacrylamide)indolines HDAC inhibitors exhibit potent anti-inflammatory activity. HDAC inhibitors suppress cytokine in vitro and in vivo: A panel of HDAC inhibitors was developed and evaluated for anti-inflammatory activity, which has not been well studied previously. Compound 1 was more potent than SAHA in vitro and in vivo. Our results suggest that 1 is a novel agent for the treatment of inflammation-associated diseases. Copyright ? 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.[SDGs]SDG33 (1 benzenesulfonyl 1h indol 5 yl) n hydroxyacrylamide; 3 [1 (4 methoxybenzenesulfonyl) 2,3 dihydro 1h indol 5 yl] n hydroxyacrylamide; antiinflammatory agent; cyclooxygenase 2; histone deacetylase inhibitor; indometacin; inducible nitric oxide synthase; interleukin 6; prostaglandin E2; tumor necrosis factor alpha; unclassified drug; vorinostat; animal experiment; animal model; antiinflammatory activity; antiproliferative activity; article; controlled study; cytokine production; cytokine release; IC 50; nonhuman; priority journal; protein expression; rat; Wittig reaction; anti-inflammatory agents; gene expression; histone deacetylase; indolines; inhibitors; Acrylamides; Animals; Anti-Inflammatory Agents; Cytokines; HeLa Cells; Histone Deacetylase Inhibitors; Humans; Indoles; Male; Mice; Rats; Rats, Wistar; Structure-Activity Relationship; Rattusjournal article10.1002/cbic.201300201237882542-s2.0-84879840340