Discovery of Ureido-Based Apcin Analogues as Cdc20-specific Inhibitors against Cancer.

ABSTRACT: Cdc20 is a promising drug target that plays an important role in the mid-anaphase process of cellular mitosis, and Apcin is the only reported core structure of the Cdc20-specific inhibitor. Some potent Apcin derivatives were obtained in our previous research, and a structure-activity relationship was determined. In this study, we designed and synthesized a series of ureido-based Apcin derivatives. The proliferation-inhibition experiments on four cancer-cell lines showed that ureido skeleton could promote the anti-proliferation activity of purine-substituted compounds, whereas the ureido analogues with pyrimidine substitutes showed no significant improvement in the inhibitory effect compared with the original ones. Further tests confirmed that ureido-based compounds can enhance the binding

SUBMITTER: He Y 

PROVIDER: S-EPMC9964651 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature