Protolichesterinic acid derivatives: α-Methylene-γ-lactones as potent dual activators of PPARγ and Nrf2 transcriptional factors
作者: Anne-Cécile Le LamerHélène AuthierIsabelle RouaudAgnès CosteJoël BoustieBernard PipyNicolas Gouault
作者单位: 1Equipe PNSCM, UMR CNRS 6226, Université de Rennes 1, 2 Avenue du Pr. Léon Bernard, F-35043 Rennes, France
2Université de Toulouse III, 118, Route de Narbonne, F-31062 Toulouse Cedex 09, France
3Université de Toulouse III, UPS, PHARMA-DEV, UMR 152, 118, Route de Narbonne, F-31062 Toulouse Cedex 9, France
4IRD, UMR 152, F-31062 Toulouse Cedex 9, France
刊名: Bioorganic & Medicinal Chemistry Letters, 2014, Vol.24 (16), pp.3819-3822
来源数据库: Elsevier Journal
DOI: 10.1016/j.bmcl.2014.06.062
关键词: Protolichesterinic acidα-Methylene-γ-lactonesMichael acceptorNrf2PPARγ
英文摘要: Abstract(#br)PPARγ and Nrf2 are important transcriptional factors involved in many signaling pathways, especially in the anti-infectious response of macrophages. Compounds bearing a Michael acceptor moiety are well known to activate such transcriptional factors, we thus evaluated the potency of α,β-unsaturated lactones synthesized using fluorous phase organic synthesis. Compounds were first screened for their cytotoxicity in order to select lactones for PPARγ and Nrf2 activation evaluation. Among them, two α-methylene-γ-lactones were identified as potent dual activators of PPARγ and Nrf2 in macrophages.
全文获取路径: Elsevier  (合作)
影响因子:2.338 (2012)

  • acceptor 收体
  • derivatives 派生物
  • potent 强大的