In breast and certain other cancers, receptor tyrosine kinases, including the insulin-like growth factor I receptor (IGF-IR), play an important role in promoting the oncogenic process. The IGF-IR is therefore an important target for developing new anti-breast cancer therapies. An initial screening of a chemical library against the IGF-IR in breast cancer cells identified a diaryl urea compound ...

N-Benzyl- and N-2°-alkylpyridinium salts were engaged in visible-light-driven, photoredox-induced radical-cationic three-component couplings with N-methylmaleimide acrylonitrile as radical acceptors, combination 1,1-diarylethylenes donor alkenes. These multicomponent coupling reactions could be achieved under mild conditions, high efficiency, to furnish diverse 3,4-disubstituted pyrrolidin-2,5-...

Gas-phase activation data were obtained for model sulfoxide elimination reactions. The activation enthalpy for methyl 3-phenylpropyl sulfoxide is 32.9 +/- 0.9 kcal/mol. Elimination by methyl vinyl sulfoxide to form acetylene has an enthalpic barrier of 41.6 +/- 0.8 kcal/mol and that of 3-phenylpropyl methanesulfinate to form hydrocinnamaldehyde is 34.6 +/- 0.6 kcal/mol. Calculations at the MP2/...

Methionine residues in protein can be oxidized by reactive oxygen or nitrogen species to generate methionine sulfoxide. This covalent modification has been implicated in processes ranging from normal cell signaling to neurodegenerative diseases. A general method for detecting methionine sulfoxide in proteins would be of great value in studying these processes, but development of a chemical or i...

Application of dimethyl sulfoxide to proliferating L8 myoblasts (an established cell line of rat skeletal muscle) for 72 hr completely prevented fusion and induction of creatine phosphokinase (EC 2.7.3.2) activity (an indicator of muscle differentiation). The growth pattern changed from the usual sheets of randomly oriented cells to flattened, whorled monolayers of elongated fibroblast-like cel...

A 1H NMR study of urocanic acid dissolved in water/dimethyl sulfoxide mixtures together with potentiometric determinations of its two successive acidities in the same solutions reveal that a proton is transferred from the imidazolium ring to the carboxylate group when the amount of dimethyl sulfoxide is increased. An analysis of the potentiometric data by means of the classical Hammett linear r...

Friend murine erythroleukemia cells underwent apparently normal erythropoiesis when treated with dimethyl sulfoxide. One of the earliest events associated with this induction was a decrease in ouabain sensitive 86Rb+ uptake, an assay of the plasma membrane Na,K(ATPase). Ammonium vanadate (10 microM) blocked differentiation of these cells without affecting cell viability. Vanadium was taken up b...