Design and Synthesis of New Hydantoin Acetanilide Derivatives as Anti-NSCLC Targeting EGFR^L858R/T790M Mutations.

ABSTRACT: Epidermal Growth Factor Receptor (EGFR), its wild type and mutations L858R/T790M, is overexpressed in non-small cell lung cancer (NSCLC) patients and is considered an inevitable oncology target. However, while the potential EGFR inhibitors have been represented in the literature, their cellular activity failed to establish broad potency against EGFR and its mutations. This study identifies a new series of EGFR^L858R/T790M inhibitors bearing hydantoin acetanilides. Most compounds revealed strong antiproliferative activity in a range of NSCL cancer models (A549, H1975, and PC9), in which 5a and 5f were the most potent. Compounds 5a and 5f possessed potent anticancer activity on H1975 cells with IC₅₀ values of 1.94 and 1.38 µM, respectively, co

SUBMITTER: Hassanin MA 

PROVIDER: S-EPMC9317481 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature