Dear colleagues,
I would like to invite you to the lecture by Antonio Conte called "Targeting DYRK1A with Purpose: A Multicomponent Strategy for Selective Covalent Inhibition via Triazolopiperazine Scaffolds". The lecture will be on Wednesday April 9, 2025 at 9AM in room 1.09 at IMTM.
Abstract
DYRK1A is a challenging but promising target in neurodegeneration and cancer. We present a modular multicomponent reaction (MCR) strategy to develop selective covalent inhibitors based on a triazolopiperazine scaffold. This core is further diversified into tetrazole derivatives, enabling fine-tuned binding and potential macrocyclization for enhanced pharmacokinetics. Our approach offers a streamlined path to structurally diverse, drug-like candidates with improved selectivity and stability.