• Biological Evaluations, NMR Analyses, Molecular Modeling Studies, and Overview of the Synthesis of the Marine Natural Product (−)-Mucosin 

      Nolsøe, Jens Mortansson Jelstrup; Underhaug, Jarl; Sørskår, Åshild Moi; Antonsen, Simen; Malterud, Karl Egil; Gani, Osman; Fan, Qiong; Hjorth, Marit; Sæther, Thomas; Hansen, Trond Vidar; H. Stenstrøm, Yngve (Journal article; Tidsskriftartikkel; Peer reviewed, 2024-02-24)
      Natural products obtained from marine organisms continue to be a rich source of novel structural architecture and of importance in drug discovery, medicine, and health. However, the success of such endeavors depends on the exact structural elucidation and access to sufficient material, often by stereoselective total synthesis, of the isolated natural product of interest. (−)-Mucosin (1), a fatty ...
    • Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist 

      Arnesen, Henriette; Haj-Yasein, Nadia N.; Tungen, Jørn E.; Soedling, Helen; Matthews, Jason; Paulsen, Steinar M.; Nebb, Hilde I.; Sylte, Ingebrigt; Hansen, Trond Vidar; Sæther, Thomas (Journal article; Tidsskriftartikkel; Peer reviewed, 2019-07-19)
      The peroxisome proliferator activated receptors (PPARs) are important drug targets in treatment of metabolic and inflammatory disorders. Fibrates, acting as PPARα agonists, have been widely used lipid-lowering agents for decades. However, the currently available PPARα targeting agents show low subtype-specificity and consequently a search for more potent agonists have emerged. In this study, previously ...
    • Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects 

      Sæther, Thomas; Paulsen, Steinar M; Tungen, Jørn Eivind; Vik, Anders; Aursnes, Marius; Holen, Torgeir; Hansen, Trond Vidar; Nebb, Hilde Irene (Journal article; Tidsskriftartikkel; Peer reviewed, 2018-06-18)
      Obesity and associated disorders such as metabolic syndrome and type 2 diabetes (T2D) have reached epidemic proportions. Several natural products have been reported as Peroxisome Proliferator-Activated Receptor (PPAR) agonists, functioning as lead compounds towards developing new anti-diabetic drugs due to adverse side effects of existing PPAR drugs. We recently isolated and identified (7E)-9-oxoh ...
    • Synthesis, biological evaluation and molecular modeling of new analogs of the anti-cancer agent 2-methoxyestradiol: potent inhibitors of angiogenesis 

      Solum, Eirik Johansson; Cheng, Jing-Jy; Sylte, Ingebrigt; Vik, Anders; Hansen, Trond Vidar (Journal article; Tidsskriftartikkel; Peer reviewed, 2015-03-27)
      The synthesis, cytotoxicity, inhibition of tubulin polymerization and anti-angiogenic effects of 10 analogs of 2-methoxyestradiol are reported. These efforts revealed that the analog with a 4-pyridine ring in the 17-position, in combination with 2-ethyl- and 3-sulfamate substituents on the steroid A-ring, is the most interesting anti-cancer agent. This compound showed potent inhibitory effects against ...
    • Synthesis, biological evaluation and molecular modeling studies of the PPARβ/δ antagonist CC618 

      Kaupang, Åsmund; Paulsen, Steinar Martin; Steindal, Calin Constantin; Ravna, Aina Westrheim; Sylte, Ingebrigt; Halvorsen, Trine Grønhaug; Thoresen, G. Hege; Hansen, Trond Vidar (Journal article; Tidsskriftartikkel; Peer reviewed, 2015-03-05)
      Abstract: Herein, we describe the synthesis, biological evaluation and molecular docking of the selective PPARb/ d antagonist (4-methyl-2-(4-(trifluoromethyl)phenyl)-N-(2-(5-(trifluoromethyl)-pyridin-2-ylsulfonyl) ethyl)thiazole-5-carboxamide)), CC618. Results from in vitro luciferase reporter gene assays against the three known human PPAR subtypes revealed that CC618 selectively antagonizes ...