Novel fluorophores: efficient synthesis and photophysical properties.

The synthesis of new donor-acceptor acetylene-bridged compounds was realized via organophosphorus reactions and Sonogashira couplings. These systems exhibit high fluorescence quantum yields, and excitation induces very efficient charge redistribution in the molecules. [structure: see text]

Discovery of highly potent Src SH2 binders: structure-activity studies and X-ray structures.

Optimization of the hydrophobic moiety of caprolactam/thiazepinone based compounds led to the identification of potent Src SH2 binders in two different series incorporating a phosphotyrosine group (RU 81843) or a phosphobenzoic group (RU 79181). The X-ray co-structures with the Src SH2 domain revealed different binding modes for RU 81843 and RU 79181, and an excellent fit between RU81843 and the Src SH2 protein thus explaining its high potency (9 nM, 15-fold more potent than pYEEI reference peptide).