Synthesis of novel spiropyrazoline oxindoles and evaluation of cytotoxicity in cancer cell lines

被引:98
作者
Monteiro, Angelo [1 ]
Goncalves, Lidia M. [1 ]
Santos, Maria M. M. [1 ]
机构
[1] Univ Lisbon, Fac Farm, Inst Invest Med iMed ULisboa, P-1649003 Lisbon, Portugal
关键词
Spirooxindole; Pyrazoline; Structure-activity relationship; Cytotoxicity; Anticancer agents; BREAST-CANCER; POTENT;
D O I
10.1016/j.ejmech.2014.04.023
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of novel spiropyrazoline oxindole derivatives was synthesized by 1,3-dipolar cycloaddition reaction. The compounds were screened for their in vitro cytotoxic activity against MCF-7 breast cancer cell line (estrogen receptor positive (ER+) and human epidermal growth factor receptor 2 negative (HER2-)). Of the nineteen spiropyrazoline oxindoles tested, six compounds have a GI(50) below 12 mu M The most potent compounds in this series were also evaluated against MDA-MB-231 breast cancer cell line (ER and HER2-). Two spiropyrazoline oxindoles were highly selective between MCF-7 tumor cells and MDA-MB-231 tumor cells. More importantly, they were noncytotoxic against HER 293T non tumor derived cell lines. (c) 2014 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:266 / 272
页数:7
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