Chiral poly(thiophenes) have been synthesized by electropolymerization; they exhibit high specific rotation, stability, and conductivity and can stereoselectively recognize chiral anions used as doping agents during voltammetric cycles.
Rose Bengal, a dye sensitizer, was found to be active as a visible light photoredox catalyst for the direct enantioselective α-alkylation of aldehydes in environmentally benign and simple conditions. Starting from a SOMO converse mechanism, the catalytic activity of the imidazolidinone organocatalyst was improved using an electrophilic cocatalyst. The resulting methodology and optimal conditions led to efficient and transition-metal-free direct photoredox organocatalysis.Scheme 1 Previous laboratory work showing the competitive pathways in the photo-oxidation of tertiary amines. † Electronic supplementary information (ESI) available: General procedures, experimental data, photosensitizers properties, spectroscopic data. See
DNA methyltransferases (DNMTs) are responsible for DNA methylation, an epigenetic modification involved in gene regulation. Families of conjugates of procainamide, an inhibitor of DNMT1, were conceived and produced by rapid synthetic pathways. Six compounds resulted in potent inhibitors of the murine catalytic Dnmt3A/3L complex and of human DNMT1, at least 50 times greater than that of the parent compounds. The inhibitors showed selectivity for C5 DNA methyltransferases. The cytotoxicity of the inhibitors was validated on two tumour cell lines (DU145 and HCT116) and correlated with the DNMT inhibitory potency. The inhibition potency of procainamide conjugated to phthalimide through alkyl linkers depended on the length of the linker; the dodecane linker was the best.
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