Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 73, Issue -, Pages 153-166Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.11.034
Keywords
Selenium; Antiproliferatives; Cytotoxicity; Cancer
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Funding
- Ministerio de Educacion y Ciencia, Spain [SAF 2009-07744]
- CAN Foundation
- University of Saarland
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A series of 31 new selenoesters were synthesized and their cytotoxic activity was evaluated against a prostate cancer cell line (PC-3). The most active compounds were also tested against three tumoural cell lines (MCF-7, A-549 and HT-29) and one non-tumour prostate cell line (RWPE-1). Thirteen compounds showed significant activity towards all tumour cells investigated, and some of them were even more potent than etoposide and cisplatin, which were used as reference drugs. Because of their pronounced potency and/or selectivity, four analogues (5, 21, 28 and 30), were selected in order to assess their redox properties related to a possible redox modulating activity. The glutathione peroxidase (GPx) assay showed slight activity for compound 30 and the 2,2-dipheny1-1-picrylhydrazyl-(DPPH) assay showed a weak activity for compounds 5 and 28. The present results revealed that analogues 5, 21, 28 and 30 might serve as a useful starting point for the design of improved anti-tumour agents. (C) 2013 Elsevier Masson SAS. All rights reserved.
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