Nikolett Péczka

Fragment‐Based Screening of Heterocyclic Electrophiles Identified Acrylamide Bioisoteres for Covalent KRasG12C Inhibitors

Covalent fragment approaches gained increasing attention in medicinal chemistry. Our covalent heterocyclic fragment library (Covalent MiniFrags) consisting of five and six membered heterocycles was screened against the oncogenic target KRasG12C. First, we detected the labeling of cysteine residues by Ellman's free thio...