Synthesis and Cytotoxicity of Amino-Pyrazole Derivatives with Preliminary SAR

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

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 2 , 2017

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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).

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

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Article Details

VOLUME: 14
ISSUE: 2
Year: 2017
Page: [151 - 158]
Pages: 8
DOI: 10.2174/1570180813666160930162522
Price: $65

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