详细信息
文献类型:期刊文献
英文题名:Design, Synthesis, and Biological Evaluation of Pyrazole Derivatives
作者:Hu, Chunqi[1];Gao, Yali[1];Du, Wenting[2]
机构:[1]Shaoxing Univ, Coll Chem & Chem Engn, Shaoxing 312000, Peoples R China;[2]Zhejiang Med Coll, Dept Pharm, 481 Binwen Rd, Hangzhou 310053, Zhejiang, Peoples R China
年份:2016
卷号:87
期号:5
起止页码:673
外文期刊名:CHEMICAL BIOLOGY & DRUG DESIGN
收录:SCI-EXPANDED(收录号:WOS:000374031500003)、、Scopus(收录号:2-s2.0-84954135167)、WOS
基金:This study was financially supported by Zhejiang Provincial Natural Science Foundation (No. LY16H300004 and No. LQ13H300001), the Natural Science Foundation of China (No. 81502926). 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:anticancer; molecular docking; p53-MDM2; pyrazole derivatives; synthesis
外文摘要:In this in vitro study, a series of novel pyrazole derivatives were designed, synthesized, and evaluated against five human cancer cell lines (PC3, A549, HL60, HCT116, and SW620) for their antiproliferative and p53-MDM2 binding inhibitory activities. Although biological evaluations showed that this series of compounds possessed weak p53-MDM2 inhibitory activities, most of them displayed moderate to potent antiproliferative activities against the tested cells lines. Compound 11c exhibited the best potency for MDM2 (FP-IC50 = 29.22 m) and demonstrated antiproliferative activities in response to the five tested cell lines (IC50 = 4.09-16.82 m). Compared with the positive control Nutlin-1, there was enhanced antiproliferative activity to p53-mutated or p53-deficient cell lines (SW620, HL60, and PC3).
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