Blar i Institutt for kjemi på forfatter "Aarhus, Thomas Ihle"
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Evaluation of protective groups for purines in synthesis of CSF1R inhibitors
Bygdås, Håkon Steinholt (Master thesis, 2019)Kolonistimmulerende faktor 1 (CSF1) er ofte overuttrykt i flere typer kreft, betennelsessykdommer og beinsykdommer. Studier har vist at hemning av den kolonistimmulerende faktor 1 reseptor kinasen (CSF1R) kan gi økt effekt ... -
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, ... -
Investigation of 4,6-Disubstituted Pyrrolo[2,3-d]pyrimidines as Potential Colony-Stimulating Factor 1 Receptor Inhibitors; Synthesis of Carboxylic Acid Derivatives on the Aromatic Moiety at Position C-6.
Rognstad, Line (Master thesis, 2019)I medisinsk kjemi har små molekyler blitt et viktig forskningsområde innen legemidler. Fusjonerte heterosykler har blitt rapportert til å utfolde en rekke biologiske aktiviteter, og pyrrolopyrimidiner er en av hovedklassene ... -
Negishi Cross-Coupling Reaction in the Synthesis of Benzyl Substituted Pyrrolopyrimidines as CSF-1R Inhibitors
Teksum, Vilde (Master thesis, 2020) -
Palladium Catalyzed Cross-Coupling Reactions on 7-Azaindoles in the Synthesis of CSF1R Inhibitors
Selmer-Olsen, Sigrid Maria Elisabeth (Master thesis, 2019)Overuttrykk av colony stimulating factor 1 receptor (CSF1R) tyrosin kinase er blitt linket til flere sykdommer, blant annet kreft, benosteolyse og betennelseslidelser. En lovende behandlingsstrategi for disse sykdommene ... -
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 ... -
Synthesis and Pharmacological Development of Pyrrolopyrimidines and Purines as Inhibitors of the Colony Stimulating Factor 1 Receptor Tyrosine Kinase
Aarhus, Thomas Ihle (Doctoral theses at NTNU;2023:166, Doctoral thesis, 2023)Protein kinases regulate the function of virtually all fundamental cellular processes and have thus become important drug targets for modulating abnormal cellular behavior in a variety of disease states. However, the ... -
Synthetic strategies towards 4,6-disubstituted pyrrolo[2,3-d]pyrimidines as potential CSF-1R inhibitors
Tsui, Hay Man Hilde (Master thesis, 2019)Målet med denne masteroppgaven var å syntetisere nye 4,6-disubstituerte pyrrolo[2,3-d]pyrimidiner som hemmere for CSF-1R (”colony stimulating factor 1 receptor”) tyrosinkinase. En ny strategi for syntese av disse er også ...