P129, a pyrazole ring-containing isolongifolanone-derivate: synthesis and investigation of anti-glioma action mechanism.

ABSTRACT:

Background

Cyclin-dependent kinase-2 (CDK-2) is an important regulatory factor in the G₁/S phase transition. CDK-2 targeting has been shown to suppress the viability of multiple cancers. However, the exploration and application of a CDK-2 inhibitor in the treatment of glioblastoma are sparse.

Methods

We synthesized P129 based on isolongifolanone, a natural product with anti-tumor activity. Network pharmacology analysis was conducted to predict the structural stability, affinity, and pharmacological and toxicological properties of P129. Binding analysis and CETSA verified the ability of P129 to target CDK-2. The effect of P129 on the biological behavior of glioma cells was analyzed by the cell counting kit-8, colony formation, flow cytometry, and other experiments.

SUBMITTER: Jiang Y 

PROVIDER: S-EPMC10771574 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature