August 14, 2025

Design, synthesis, and biological evaluation of 5-chlorine-2-amino-pyrimidine derivatives as potent PLK4 inhibitors.

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Design shows potent PLK4 inhibition in TRIM37-amplified MCF-7 cells, suggesting promising therapeutic potential.

Compound 5f demonstrates exceptional PLK4 inhibition, with an IC50 of 0.8 nM and significant anti-proliferative activity.
Approximately half of the designed amino-pyrimidine compounds exhibited potent PLK4 inhibition, indicating diverse structural potential.
The study utilized a structure-activity relationship (SAR) approach to design and evaluate PLK4 inhibitors effectively.
These findings highlight 5f's ability to induce mitotic arrest and trigger apoptosis in cancer cells, warranting further exploration.

Mu et al. (2025) studied this question.

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