Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 79, Issue -, Pages 266-272Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.04.023
Keywords
Spirooxindole; Pyrazoline; Structure-activity relationship; Cytotoxicity; Anticancer agents
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Funding
- FCT (Fundacao para a Ciencia e a Tecnologia, Portugal) [PTDC/QUI-QUI/111664/2009, PTDC/SAU-FAR/110848/2009, PEst-OE/SAU/U14013/2014]
- Fundação para a Ciência e a Tecnologia [PTDC/SAU-FAR/110848/2009, PTDC/QUI-QUI/111664/2009] Funding Source: FCT
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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.
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