Design, nanogel synthesis, anti-proliferative activity and <i>in silico</i> ADMET profile of pyrazoles and pyrimidines as topo-II inhibitors and DNA intercalators.

ABSTRACT: Pyrazole derivatives 2 and 3, pyrimidine derivative 4, and their nanogels as drug delivery systems were synthesized, and their cytotoxicity against MCF-7, HCT-116, HepG2 and A549 cells was evaluated. Herein, we focused on the characterization and synthesis of chitosan/polyvinyl alcohol (Cs/PVA) nanogels loaded with derivatives 2, 3 and 4. The stability of the prepared nanogels 2, 3 and 4 was elucidated by zeta potential measurements, which possessed negative values of -9.7, -1.3 and -1.6 mV, respectively. Our compounds and their nanogels were evaluated as topo-II inhibitors and DNA intercalators. The nanogel delivery system enhanced the cytotoxicity of compound 2 against the A549, HCT116, HepG2 and MCF-7 cancer cell lines by 32.06%, 28.96%, 44.32% and 50.00%, respectively. Moreover, the na

SUBMITTER: Aljohani AKB 

PROVIDER: S-EPMC11960622 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature