Browsing NTNU Open by Author "Han, Jin"
Now showing items 1-9 of 9
-
Balancing potency, metabolic stability and permeability in pyrrolopyrimidine-based EGFR inhibitors
Han, Jin; Henriksen, Silje; Nørsett, Kristin Gabestad; Sundby, Eirik; Hoff, Bård Helge (Journal article; Peer reviewed, 2016)The present study describes our continuous effort to develop epidermal growth factor receptor (EGFR) inhibitors based on the 6-aryl-pyrrolo[2,3-d]pyrimidin-4-amine scaffold. The activity-ADME space has been evaluated by ... -
Identification of fused pyrimidines as interleukin 17 secretion inhibitors
Reiersølmoen, Ann Christin; Han, Jin; Sundby, Eirik; Hoff, Bård Helge (Journal article; Peer reviewed, 2018)Inhibiting the interleukin 17 pathway is of interest in a number of autoimmune diseases. Herein, 42 fused pyrimidines have been evaluated as interleukin 17 secretion inhibitors using a phenotypic assay with peripheral ... -
Investigation of Pyrrolo- and Furopyrimidines as Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors: Synthesis and Activity-ADME Profile
Han, Jin (Doctoral theses at NTNU;2016:351, Doctoral thesis, 2016)Summary of thesis: Due to their essential roles in signal transduction and regulation of cellular processes, kinases have been established as promising drug targets for the treatment of various human diseases. Since ... -
Synthesis and Biological Evaluation of Furo[2,3-d]pyrimidines as EGFR Tyrosine Kinase Inhibitors
Nervik, Sondre (Master thesis, 2015)The work performed in this master s thesis has contributed to a larger ongoing study on the development of new epidermal growth factor (EGFR) tyrosine kinase inhibitors, intended for use in cancer chemotherapy. The ... -
Synthesis of 5-Aryl-Pyrrolo[2,3-d]pyrimidines and Their Bioactivity
Reiersølmoen, Ann Christin (Master thesis, 2016)The epidermal growth factor receptor tyrosine kinase is one of the more important targets in targeted cancer therapy. However, on prolonged administration of EGFR inhibitors, resistance emerge, which in 50% of the cases ... -
Synthesis of 6-Aryl-pyrrolopyrimidines - Effect of ortho Substituents on EGFR Inhibitory Activity
Henriksen, Silje (Master thesis, 2015)The goal of this project was to synthesise new and active epidermal growth factor receptor (EGFR) inhibitors which hopefully can be used in treatment of cancer. Seven new biological active pyrrolopyrimidines have been ... -
Synthesis of Pyrrolopyrimidines as CSF-1R Kinase Inhibitors
Larsen, Kristin Uhlving (Master thesis, 2016) -
Synthesis of pyrrolopyrimidines for CSF-1R inhibition
Leithaug, Trygve (Master thesis, 2017) -
Synthesis of Pyrrolopyrimidines for Investigation of JAK2 Inhibition
Bekkevard, Pål Unnerud (Master thesis, 2015)A series of 7H-pyrrolo- and thieno[2,3-d]pyrimidine based compounds have been synthesized and tested for Janus kinase 2 (JAK2) inhibition, as part of a fragment-based approach to obtaining information on structure-activity ...