title: Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
abstract: We synthesized a series of delta-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-alpha and nitric oxide by LPS-stimulated RAW264.7 cells.
authors.affiliation: Bioevaluation Center, KRIBB, Daejeon 305-806, Korea.
authors.forename: Hwan Mook
authors.initials: HM
authors.lastname: Kim
authors.forename: Dong-Kyu
authors.initials: DK
authors.lastname: Ryu
authors.forename: Yongseok
authors.initials: Y
authors.lastname: Choi
authors.forename: Bum Woo
authors.initials: BW
authors.lastname: Park
authors.forename: Kiho
authors.initials: K
authors.lastname: Lee
authors.forename: Sang Bae
authors.initials: SB
authors.lastname: Han
authors.forename: Chang-Woo
authors.initials: CW
authors.lastname: Lee
authors.forename: Moo-Rim
authors.initials: MR
authors.lastname: Kang
authors.forename: Jong Soon
authors.initials: JS
authors.lastname: Kang
authors.forename: Shanthaveerappa K
authors.initials: SK
authors.lastname: Boovanahalli
authors.forename: Song-Kyu
authors.initials: SK
authors.lastname: Park
authors.forename: Jung Whan
authors.initials: JW
authors.lastname: Han
authors.forename: Tae-Gyu
authors.initials: TG
authors.lastname: Chun
authors.forename: Hee-Yoon
authors.initials: HY
authors.lastname: Lee
authors.forename: Ky-Youb
authors.initials: KY
authors.lastname: Nam
authors.forename: Eun Hyun
authors.initials: EH
authors.lastname: Choi
authors.forename: Gyoonhee
authors.initials: G
authors.lastname: Han
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D056572:Histone Deacetylase Inhibitors; D006801:Humans; D007769:Lactams / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D008958:Models, Molecular; D009569:Nitric Oxide / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D013329:Structure-Activity Relationship; D014183:Transplantation, Heterologous; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000096:biosynthesis
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D056572:Histone Deacetylase Inhibitors; D007769:Lactams; D008070:Lipopolysaccharides; D014409:Tumor Necrosis Factor-alpha; D009569:Nitric Oxide