Design, synthesis and molecular modeling of new coumarin-thiazole derivatives as dual EGFR/HDAC1 inhibitors: <i>in vitro</i> and <i>in vivo</i> anticancer assays.

ABSTRACT: The growing evidence ascertaining the overexpression of EGFR and HDAC1 in breast and colorectal cancers prompted us to design and synthesize some new coumarin-thiazole derivatives with dual EGFR/HDAC1 inhibitory activity, considering the nature of EGFR and HDAC inhibitory models. The new derivatives were evaluated for their in vitro cytotoxicity against HCT-116 and MCF-7 cancer cells along with BJ-1 normal cells. Compound 3-(-1-((-5-(-(4-bromophenyl)diazenyl)-4-methylthiazol-2(3H)-ylidene)hydrazono)ethyl)-4-hydroxy-2H-chromen-2-one (3m) showed promising selectivity indices for both cell lines, preferential inhibition of EGFR/HDAC1/ERK, induction of cell cycle arrest and apoptosis, and significant in vivo antitumor activity against Ehrlich ascites and solid carci

SUBMITTER: Ahmed EY 

PROVIDER: S-EPMC12423761 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature