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

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

Eur J Med Chem

Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal. Electronic address:

Published: May 2014

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 GI50 below 12 μM 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 HEK 293T non tumor derived cell lines.

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http://dx.doi.org/10.1016/j.ejmech.2014.04.023DOI Listing

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