Pyrrolizidines for Drug Design

Pyrrolizidine is a tertiary amine found in the structures of natural alkaloids and bioactive molecules. Notably, it is present in various serotonin receptor agonists/antagonists and KRAS mutant inhibitors undergoing clinical trials for anticancer therapy. For example, in the structure of MRTX1133 (Phase 1 trials), the pyrrolizidine moiety forms a nonclassical hydrogen bond with Glu62 residue when binding to the cancerogenic KRAS protein, endowing the drug with better cellular potency and selectivity. Discover our set of pyrrolizidine derivatives, homologues, and analogues!