1-(sulfonyl)-5-(arylsulfonyl)indoline as activators of the tumor cell specific M2 isoform of pyruvate kinase.

Cancer cells preferentially use glycolysis rather than oxidative phosphorylation for their rapid growth. They consume large amount of glucose to produce lactate even when oxygen is abundant, a phenomenon known as the Warburg effect. This metabolic change originates from a shift in the expression of alternative spliced isoforms of the glycolytic enzyme pyruvate kinase (PK), from PKM1 to PKM2.

Dendritic effects in catalysis by Pd complexes of bidentate phosphines on a dendronized support: Heck vs. carbonylation reactions.

Bidentate phosphine ligands have been prepared on polystyrene beads modified with polyether dendron spacers. When complexed to Pd(0), these systems exhibited a negative dendritic effect on Heck catalysis (contrary to the analogous monodentate phosphine systems), but mostly a positive influence on carbonylation. This opposite influence of the dendronization falls into line with other differences in the optimal ligand structure for the two reactions.

Polymer-supported proline-decorated dendrons: dendritic effect in asymmetric aldol reaction.

The yield and enantioselectivity of an asymmetric aldol reaction, catalyzed by a proline derivative immobilized on polystyrene via dipolar cycloaddition, are remarkably improved by the dendronization of the support.