Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 64, Issue -, Pages 529-539Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.03.045
Keywords
Sulforaphane; Cytotoxicity; Cell cycle arrest; Apoptosis; Nrf2
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Funding
- National Natural Science Foundation of China [21202012]
- Industry for Attracting Ph. D. Scientists Program of Jiangsu Province
- Changzhou Key Technology R&D Program (Society Development)
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A series of sulforaphane derivatives were synthesized and evaluated in vitro for their cytotoxicity against five cancer cell lines (HepG2, A549, MCF-7, HCT-116 and SH-SY5Y). The pharmacological results showed that many of the derivatives displayed more potent cytotoxicity than sulforaphane (SFN). Furthermore, SFN and derivative 85 could induce cell cycle arrest at S or G2/M phase and cell apoptosis. SFN and 85 exhibited time- and dose-dependent activation on Nrf2 transcription factor, and 85 acted as a more potent Nrf2 inducer than SFN. (C) 2013 Elsevier Masson SAS. All rights reserved.
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