Dual VEGFR-2 and EGFR^T790M inhibitors of phenyldiazenes: anticancer evaluations, ADMET, docking, design and synthesis.

ABSTRACT:

Aim

New phenyldiazene scaffold-linked heterocyclic pyrazole, pyrimidinone, pyrimidinthione, and/or triazine rings have been developed and synthesized.

Methods & results

Cytotoxicity of our derivatives was estimated on four cancer and VERO normal cell lines targeting EGFR^T790M (epidermal growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) enzymes. Our new derivatives selectively inhibited both VEGFR-2 and EGFR as they have the essential structural requirements for inhibitors of both receptors. Derivative 14 was the most active on A549, HCT116, HepG2, and MCF-7 cancers with half-maximal inhibitory concentration (IC₅₀) = 5.50, 9.77, 7.12, and 7.85 µM respectively. The assessed derivatives 5, 7, 8, 9,

SUBMITTER: Alsulaimany M 

PROVIDER: S-EPMC11792794 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature