Macrocyclization via Ring-Closing Metathesis in Drug Discovery & Process Chemistry
Drug Hunter
JUNE 5, 2023
Macrocyclic molecules, containing 12 or more atoms in a ring system, are increasingly prevalent in drug discovery, with over 67 macrocyclic drugs approved so far and several notable examples of clinical success highlighted on Drug Hunter recently, including MK-0616 , repotrectinib , and pacritinib. By imparting conformational restraint and reducing entropy of binding, macrocyclization can enable more potent and selective binding to targets, while simultaneously reducing rotatable bonds and hence
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