Blar i NTNU Open på forfatter "Sundby, Eirik"
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Improved Synthetic Methodology, Substrate Scope and X-ray Crystal Structure for N, N’-disubstituted Guanidines
Elumalai, Vijayaragavan; Eigner, Václav; Visnes, Torkild; Sundby, Eirik; Hoff, Bård Helge (Peer reviewed; Journal article, 2024)Guanidine is a privileged scaffold in drug discovery. Herein we report our investigations into the acid promoted amination of pyrimidine-bearing cyanamide to produce N, N’-disubstituted guanidines. Hydrochloric acid was ... -
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 ... -
Investigation of Heck coupling on 6-bromo[2,3-d]thienopyrimidines for construction of new EGFR inhibitor lead structures
Bugge, Steffen; Sundby, Eirik; Hoff, Bård Helge; Bysting, Fredrik (Journal article; Peer reviewed, 2017)With the aim of identifying new lead structures for EGFR inhibition, a study of palladium catalysed Heck coupling between (R)-6-bromo-N-(1-phenylethyl)thieno[2,3-d]pyrimidin-4-amine and various acrylates was performed. The ... -
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 ... -
Is literature data useful for identifying enzyme catalysts for new substrates? A case study on reduction of 1-aryl-2-alkanoates
Hoff, Bård Helge; Sundby, Eirik (Journal article; Peer reviewed, 2017)The use of literature data to identify catalysts for a novel transformation is a commonly used approach. Herein, we have evaluated if this is a viable strategy in enzyme catalysis, using asymmetric reduction of 1-aryl-2-alkanoates ... -
Kartlegge og prosjektere mulig løsning for overvåkning av feilseparering av jernmalm i magnetseparator.
Svendsen, Kristoffer Aaen (Bachelor thesis, 2023)Hensikten med denne oppgaven er å kartlegge og projisere mulige løsninger for å overvåke feilseparering ved magnetisk separasjonsteknikk av jernmalm. Problemet når det oppstår feilseparering er tap av magnetisk jern ut i ... -
Kartlegging og analyse på dannelse av iso-forbindelser ved co-prosessering av bio-olje i et dieselprosessanlegg
Lauvås, Marte; Remmen, Iselin Steensen; Skjæveland, Lene (Bachelor thesis, 2022)Formålet med denne bacheloroppgaven var å analysere og kartlegge hvordan innblanding av bio-olje i et dieselprosessanlegg med deWax-katalysator og ulik reaktortemperatur vil påvirke karbonnummer og mengde iso-forbindelser ... -
Kartlegging og analyse på dannelse av iso-forbindelser ved co-prosessering av bio-oljer i et dieselprosessanlegg
Lauvås, Marte; Remmen, Iselin Steensen; Skjæveland, Lene (Bachelor thesis, 2022)Formålet med denne bacheloroppgaven var å analysere og kartlegge hvordan innblanding av bio-olje i et dieselprosessanlegg med deWax-katalysator og ulik reaktortemperatur vil påvirke karbonnummer og mengde iso-forbindelser ... -
Korrelasjon mellom livsstadie, lipidinnhold og akkumulering av polysykliske aromatiske hydrokarboner (PAH) i rognkjeks (Cyclopterus lumpus) embryo eksponert for produsert vann
Knutsen, Hannah Marie; Skarpnord, Kaja Skyrud (Bachelor thesis, 2019)Hensikten med denne bacheloroppgaven var å studere korrelasjonen mellom livsstadier, lipidsammensetning og bioakkumulering av polysykliske aromatiske hydrokarboner (PAH) i fiskearten rognkjeks (Cyclopterus lumpus). Arbeidet ... -
Lipase Catalysed Kinetic Resolution of Stiripentol
Jacobsen, Elisabeth Egholm; Anthonsen, Thorleif; El-Behairy, Mohammed Farrag; Sundby, Eirik; Aboul-Enein, Mohamed Nabil; Attia, Mohamed Ibrahim; El-Azzouny, Aida Abd El-Sattar; Amin, Kamilia M.; Abdel-Rehim, Mohamed (Journal article; Peer reviewed, 2012)Kinetic resolution of rac-Stiripentol, catalysed by lipase A from Candida antarctica by esterification with vinyl butanoate was performed with an E-value of 24. This allowed isolation of (3S)-Stiripentol with an ee of 86 ... -
Literature review on Nitrosamines – Formation, Health and Environmental Impact and the Ways of Monitoring and Analysis
Smalberget, Kristin (Bachelor thesis, 2021)International Agency for Research on Cancer (IARC) har klassifisert mer enn 10 nitrosaminer som kreftfremkallende, sannsynligvis eller muligens kreftfremkallende for mennesker. Sekundære nitrosaminer er stabile forbindelser ... -
Molecular Dynamics Analysis of Enantioselective Mechanism of Chiral Thieno-, Furo-, and Pyrrolopyrimidine Kinase Inhibitors of EGFR
Henriksen, Magnus Aleksander (Master thesis, 2020)Epidermal growth factor receptor (EGFR) inhibitors interrupt EGFR-dependent cellular signaling pathways that lead to accelerated cancerous tumor growth and proliferation, and are actively developed for treatment of various ... -
One-step lipase-catalysed preparation of eslicarbazepine
El-Behairy, Mohammed Farrag; Sundby, Eirik (Peer reviewed; Journal article, 2016)The antiepileptic eslicarbazepine (S-licarbazepine) has been prepared in one step from its racemic form RS-licarbazepine via lipase catalysed kinetic resolution. A novel stereoselective simultaneous HPLC separations of ... -
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 ... -
Syntese av referanse standarder for kvartære ammonium stoffer (QUATS)
Bang, Brage (Bachelor thesis, 2022)I dette prosjektet ble elleve kvartære ammonium stoffer (QUATS) syntetisert for bruk som referansestandarder. ˚Atte av disse stoffene tilhører gruppen dialkyldimetylammonium klorider (DDACs) og tre tilhører gruppen ... -
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 Evaluation of Azaoxindoles and Pyrrolopyrimidines as Antibacterial Agents
Blindheim, Fredrik Heen (Doctoral theses at NTNU;2022:167, Doctoral thesis, 2022)Antimicrobial resistance is a global problem. Since the end of the golden age of antibiotics in the 1970s, few new antibiotics have been developed and most of these belong to established classes of drugs. As the world’s ... -
Synthesis and Evaluation of Imidazopyridinones, Pyrrolopyrimidines and Tetrahydrocarbazoles as Antibacterial Agents
Olsen, Cecilie Elisabeth (Doctoral theses at NTNU;2024:129, Doctoral thesis, 2024)Mankind is in a continual arms race against bacteria, as we develop new antibiotics whilst the bacteria develop resistance against them. The need to produce novel antibiotics is now dire, as most new commercial antibiotics ... -
Synthesis and evaluation of pyrrolo-, thieno- and furopyrimidines as epidermal growth factor receptor tyrosine kinase inhibitors
Kaspersen, Svein Jacob (Doktoravhandlinger ved NTNU, 1503-8181; 2014:223, Doctoral thesis, 2014)Cancer is one of the leading causes of deaths around the world today and there is a high demand for new and improved drugs. Traditional cancer therapy uses chemicals that don’t differentiate between good and bad cells ...