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..
Letters in Drug Design & Discovery
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).
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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
DOI https://dx.doi.org/10.2174/1570180813666160930162522 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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