Novel curcumin-based analogues as potential VEGFR2 inhibitors with promising metallic loading nanoparticles: synthesis, biological evaluation, and molecular modelling investigation.

ABSTRACT: VEGFR2 inhibition has been established as a therapeutic approach for managing cancer. A series of curcumin-based analogues were designed, synthesized, and screened for their anticancer activity against MCF-7 and HepG-2 cell lines and WISH normal cells. Compounds 4b, 4d, 4e, and 4f showed potent cytotoxicity against MCF-7 with IC₅₀ values of 0.49, 0.14, 0.01, and 0.32 μM, respectively, compared to curcumin (IC₅₀ = 13.8 μM) and sorafenib (IC₅₀ = 2.13 μM). Interestingly, compound 4e, the most active compound, exhibited potent VEGFR2 inhibition with an IC₅₀ value of 11.6 nM (96.5% inhibition) compared to sorafenib with an IC₅₀ value of 30 nM (94.8% inhibition). Additionally, compound 4e significantly induced apoptotic cell death in MCF-7 c

SUBMITTER: Yassen ASA 

PROVIDER: S-EPMC11428034 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature