• A highly selective purine-based inhibitor of CSF1R potently inhibits osteoclast differentiation 

      Aarhus, Thomas Ihle; Eickhoff, Jan; Klebl, Bert; Unger, Anke; Boros, Johanna; Choidas, Axel; Zischinsky, Mia-Lisa; Wolowczyk, Camilla Izabel; Bjørkøy, Geir; Sundby, Eirik; Hoff, Bård Helge (Peer reviewed; Journal article, 2023)
      The colony-stimulating factor 1 receptor (CSF1R) plays an important role in the regulation of many inflammatory processes, and overexpression of the kinase is implicated in several disease states. Identifying selective, ...
    • Potent and selective EGFR inhibitors based on 5-aryl-7H-pyrrolopyrimidin-4-amines 

      Reiersølmoen, Ann Christin; Aarhus, Thomas Ihle; Eckelt, Sarah; Nørsett, Kristin Gabestad; Sundby, Eirik; Hoff, Bård Helge (Journal article; Peer reviewed, 2019)
      The epidermal growth factor receptor represents an important target in cancer therapy, and low molecular weight inhibitors based on quinazolines have reached the marked. Herein we report on a new scaffold, 5-aryl-7H-pyrr ...
    • Pyrrolopyrimidine based CSF1R inhibitors: Attempted departure from Flatland 

      Bjørnstad, Frithjof Andreas; Havik, Simen; Aarhus, Thomas Ihle; Mahdi, Iktedar; Unger, Anke; Habenberger, Peter; Degenhart, Carsten; Eickhoff, Jan; Klebl, Bert M.; Sundby, Eirik; Hoff, Bård Helge (Peer reviewed; Journal article, 2024)
      The colony-stimulating factor 1 receptor (CSF1R) is an attractive target for inflammation disorders and cancers. Based on a series of pyrrolo[2,3-d]pyrimidine containing two carbo-aromatic rings, we have searched for new ...
    • Synthesis and Development of Highly Selective Pyrrolo[2,3-d]pyrimidine CSF1R Inhibitors Targeting the Autoinhibited Form 

      Aarhus, Thomas Ihle; Bjørnstad, Frithjof Andreas; Wolowczyk, Camilla Izabel; Larsen, Kristin Uhlving; Rognstad, Line; Leithaug, Trygve; Unger, Anke; Habenberger, Peter; Wolf, Alexander; Bjørkøy, Geir; Pridans, Clare; Eickhoff, Jan; Klebl, Bert; Hoff, Bård Helge; Sundby, Eirik (Peer reviewed; Journal article, 2023)
      Colony-stimulating factor-1 receptor (CSF1R) is a receptor tyrosine kinase that controls the differentiation and maintenance of most tissue-resident macrophages, and the inhibition of CSF1R has been suggested as a possible ...