文献类型：期刊文献

英文题名：Synthesis and Cytotoxicity of Amino-Pyrazole Derivatives with Preliminary SAR

作者：Hu, Chunqi;Shen, Jianfeng[4];Du, Wenting[2,3]

机构：[1]Shaoxing Univ, Coll Chem & Chem Engn, Shaoxing 312000, Peoples R China;[2]Hangzhou Med Coll, Dept Pharm, 481 Binwen Rd, Hangzhou 310053, Zhejiang, Peoples R China;[3]Wenzhou Med Univ, Wenzhou 325035, Peoples R China;[4]Zhejiang Zhenyuan Pharmaceut, Shaoxing 312000, Peoples R China

年份：2017

卷号：14

期号：2

起止页码：151

外文期刊名：LETTERS IN DRUG DESIGN & DISCOVERY

收录：SCI-EXPANDED(收录号：WOS:000395673500004)、、Scopus(收录号：2-s2.0-85045013806)、WOS

基金：This study was financially supported by Zhejiang Provincial Natural Science Foundation (No. LY16H300004 and LQ13H300001) and the Natural Science Foundation of China (No. 81502926 and 21002026). We are also grateful to the support provided by Zhejiang Provincial Program for the Cultivation of High-level Innovative Health Talents (2014) and The 151 Talents Project in new century in Zhejiang Province (the third level, 2011).

语种：英文

外文关键词：Amino-pyrazole derivatives; synthesis; anti-cancer; p53-MDM2

外文摘要：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 mu M). Compound 8e demonstrated a comprehensive potency (FP-IC50 = 15.34 mu M) and anti-proliferative activity in all five of the cell lines tested (IC50 = 12.20-32.19 mu M).