Design and Synthesis of New Dihydropyrimidine Derivatives with a Cytotoxic Effect as Dual EGFR/VEGFR-2 Inhibitors.

ABSTRACT: We developed and synthesized tetrahydropyrimidine derivatives as possible cytotoxic agents to inhibit EGFR and VEGFR-2 in the present study. Our study completely assesses the cytotoxic efficiency of pyrimidine-based derivatives 4-15 against various cancer cell lines, revealing derivatives 12 and 15 for their remarkable activity with GI₅₀ values of 37 and 35 nM, respectively, when compared to the reference erlotinib (33 nM). In vitro enzyme assays showed that target compounds, particularly 12, 14, and 15, effectively inhibited EGFR and VEGFR-2. In vitro enzyme testing revealed that compound 15 was the most promising, with IC₅₀ values of 84 and 3.50 nM for EGFR and VEGFR-2, respectively. Additionally, an in vitr

SUBMITTER: Al-Wahaibi LH 

PROVIDER: S-EPMC11325413 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature