Synthesis and Cytotoxicity of Amino-Pyrazole Derivatives with Preliminary SAR

Title:Synthesis and Cytotoxicity of Amino-Pyrazole Derivatives with Preliminary SAR

Volume: 14 Issue: 2

Author(s): Chunqi Hu, Jianfeng Shen and Wenting Du

Affiliation:

Keywords: Amino-pyrazole derivatives, synthesis, anti-cancer, p53-MDM2..

Abstract: 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).

Cite this article as:

Hu Chunqi, Shen Jianfeng and Du Wenting, Synthesis and Cytotoxicity of Amino-Pyrazole Derivatives with Preliminary SAR, Letters in Drug Design & Discovery 2017; 14 (2) . https://dx.doi.org/10.2174/1570180813666160930162522