In this in vitro study, a series of amino-pyrazole derivatives were designed, synthesized,
and evaluated against five human cancer cell lines (PC3, A549, HL60, HCT116, and SW620) for
their anti-proliferative effects and inhibition of p53-MDM2 binding. The results of the biological
evaluation showed that this series of compounds has improved inhibition of p53-MDM2 binding
and anti-proliferative activities compared to previously designed pyrazole derivatives. Compound
6e exhibited the best potency for MDM2 inhibition (FP-IC50 = 9.83 μM). Compound 8e demonstrated
a comprehensive potency (FP-IC50 = 15.34 μM) and anti-proliferative activity in all five of
the cell lines tested (IC50 = 12.20-32.19 μM).