The authors wish to replace the 'Author Contributions' statement and the affiliation for Jochen Maurer of this article [...
View Article and Find Full Text PDFBackground: Triple-negative breast cancer (TNBC) lacks biomarkers for targeted therapy. Auger emitters display the best therapeutic effect, if delivered directly into the nucleus proximal to DNA. The nuclear protein Poly (ADP-ribose)-Polymerase 1 (PARP1) is a suitable target against which few inhibitors (PARPi) are clinically approved for treatment of breast cancer with germline BRCA mutation (BRCA).
View Article and Find Full Text PDFHere, we report the first mechanochemical synthesis of sulfonimidamides. The one-pot, two-step method requires neither a solvent nor inert conditions. In a mixer mill, sulfinamides are rapidly converted to sulfonimidoyl chlorides by oxidative chlorination with -chlorosuccinimide (NCS).
View Article and Find Full Text PDFPARP1 inhibitors (PARPi) are currently approved for BRCA metastatic breast cancer, but they have shown limited response in triple negative breast cancer (TNBC) patients. Combination of an Auger emitter with PARPis enables PARP inhibition and DNA strand break induction simultaneously. This will enhance cytotoxicity and additionally allow a theranostic approach.
View Article and Find Full Text PDF2,2,2-Trifluoroethyl-substituted 3-oxazolines, 3-thiazolines, and 5,6-dihydro-2-1,3-oxazines have been obtained by reacting substituted vinyl azides with a combination of Togni's reagent and substoichiometric amounts of iron(II) chloride. The results of density functional theory calculations support the proposed mechanism involving 1,-hydrogen-atom transfer reactions.
View Article and Find Full Text PDFAn atom transfer radical addition elimination (ATRE) reaction of terminal alkenes with perfluoroalkyl halides under visible light is described. The photoredox catalysis with Eosin Y provides perfluoroalkenes in good yields. The reaction has been utilized for the late stage perfluoroalkenylation of an estrone-derived alkene.
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