Recorded: December, 2024

This webinar will review the emergence of macrocycles as a powerful strategy in drug design and discovery, highlighting the principles of rational design and the benefits and challenges of this class of compounds.

Agenda:

  • Introductions to macrocycles
    • What are macrocyclic drugs?
    • What are their advantages compared to their acyclic counterparts?
  • Macrocycle rational design
    • What are the strategies to design successful macrocycles?
    • What are the known principles for the optimization of physicochemical properties?
  • Case Study: the discovery of a novel series of PKCθ inhibitors with exquisite potency and isoform selectivity
    • Success and challenges throughout the lead optimization process