Design, synthesis, and biological investigations of new pyrazole derivatives as VEGFR2/CDK-2 inhibitors targeting liver cancer.

ABSTRACT: New Series of N-Manniche bases 3,4 (a-c) and 5,6 (a-b) were synthesized through the reaction of benzaldehyde and amine with 3-methyl-4-(aryldiazenyl)-1H-pyrazol-5-ol derivatives 2(a-c), they were fully characterized by FT-IR, (¹H, ¹³C) NMR data in addition to their mass spectra. The Structural Activity Relationship of the target compounds were examined for their cytotoxicity. Some newly synthesized compounds showed promising antiproliferation properties when tested against HepG2 cancer cells. Compounds 4a, 5a, and 6b showed potent cytotoxicity against HepG2 with IC₅₀ values of 4.4, 3.46 and 2.52 µM compared to Sorafenib (IC₅₀ = 2.051 µM) and Roscovitine (IC₅₀ = 4.18 µM). Furthermore, they were safe against the THLE2 cells with higher I

SUBMITTER: Salem MG 

PROVIDER: S-EPMC11520136 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature