Events

In this study, a series of N,O-chelated azine-enol boron complexes featuring four different fusion patterns between the benzene and pyridine rings of the azine fragment was synthesized and characterized. The optical properties of the corresponding complexes have been assessed in dichloromethane solution and in solid state. In the latter case the assessment was performed for both powder samples as well as batches of single crystals allowing to identify several cases of mechanochromism and one case of polymorphism-dependent emission.

This lecture charts future perspective in the field, while bringing attention to the countless possibilities available by diversifying not only the metal, but also the reactivity modes and tactics to bring peptide functional groups together and produce structurally diverse macrocycles.

This lecture highlights the development of a methodology that provides a repertoire of synthetic tools for the achievement of N-alkylated, macrocyclic peptides, including inhibitors of protein-protein interactions, antibacterial and anticancer peptides. The lecture also reports on the determination of the three-dimensional structures of the macrocyclic peptide serving a mimetics of protein secondary structures. This includes a detailed NMR study (i.e., TOCSY, COSY, HSQC HMBC, and ROESY) combined with molecular dynamic simulation.

In this lecture, we describe novel all-on-resin strategies permitting the synthesis of super potent (nano- and picomolar) tubulysin and dolastatin analogs and their functionalization with cleavable linkers that allow their traceless release after the selective internalization into cancer cells. We also present synthetic methods towards novel targeting peptides and their conjugates to the cytotoxic payloads.