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Full-Text Articles in Medicine and Health Sciences
Binding-Induced, Turn-On Fluorescence Of The Egfr/Erbb Kinase Inhibitor, Lapatinib, James N. Wilson
Binding-Induced, Turn-On Fluorescence Of The Egfr/Erbb Kinase Inhibitor, Lapatinib, James N. Wilson
James N Wilson
We report the photophysical properties, binding-induced turn-on emission, and fluorescence imaging of the cellular uptake and distribution of lapatinib, an EGFR/ERBB inhibitor. Lapatinib, a type II, i.e. inactive state, inhibitor that targets the ATP binding pocket of the EGFR family of receptor tyrosine kinases. DFT calculations predict that the 6-furanylquinazoline core of lapatinib should exhibit an excited state with charge transfer character and an S0 to S1 transition energy of 3.4 eV. Absorption confirms an optical tran- sition in the near UV to violet, while fluorescence spectroscopy shows that photoemission is highly sensi- tive to solvent polarity. The hydrophobicity of …
Synthesis And Evaluation Of Substituted Coumarin Derivatives As Inhibitors Of Monoamine Oxidase B, Ian A. Kieffer
Synthesis And Evaluation Of Substituted Coumarin Derivatives As Inhibitors Of Monoamine Oxidase B, Ian A. Kieffer
Chemistry Theses
Monoamine oxidase B (MAO B) is of clinical importance due to its perceived role in neurodegenerative diseases such as Parkinson’s, making inhibitors of MAO B popular candidates for drug design. A series of coumarin derivatives have been prepared and assayed, revealing that the synthesized inhibitors act through a competitive mode of inhibition. In addition, these inhibitors are potent with Ki values in the nanomolar range. Overall, substitution at the 3- position of the coumarin was found to be important to inhibitor potency and further study of 3-aryl coumarin substitution computationally led to the prediction of 3-(3-aminophenyl)-6-hydroxycoumarin as a lead compound …