Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 157, Issue -, Pages 101-114Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.07.058
Keywords
4H-chromenes; Chalcones; Michael addition; Anticancer activity; Breast cancer
Categories
Funding
- University of Minho
- Fundacao para a Ciencia e a Tecnologia
- FEDER-COMPETE through Centro de Quimica [UID/QUI/00686/2013, UID/QUI/0686/2016]
- National Program for Scientific Re-equipment [REDE/1517/RMN/2005]
- POCI 2010 (FEDER)
- FCT
- Northern Portugal Regional Operational Program (NORTE 2020), through the European Regional Development Fund (FEDER) [NORTE-01-0145-FEDER-000013]
- Competitiveness Factors Operational Program (COMPETE)
- Foundation for Science and Technology [POCI-01-0145-FEDER-007038]
- [SFRH/BPD/79609/2011]
- [SFRH/BPD/90533/2012]
- [SFRH/BD/87139/2012]
- [SFRH/BD/128850/2017]
- [PPBI-POCI-01-0145-FEDER-022122]
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Chalcone and chromene derivatives were synthesized in good yield through simple and effective reactions using innocuous solvents such as water and ethanol and high yielding aldol condensations. Generally, the reactions were performed at room temperature, leading to the isolation of highly pure compounds. These compounds were tested on breast cancer cells (MCF-7 and Hs578T) and breast nonneoplastic cells (MCF-10A). After determination of IC50 value, specific assays were performed to analyze the potential of these compounds, and those bearing halogenated substituents presented enhanced activity comparing to methoxyl or methyl groups. More specifically, the bromine atom was often present in the bioactive molecules that proceeded to the final assays and showed to be promising candidates for further studies. The selected chromene acted as a cell migration inhibitory agent and triggered regulated cell death associated with G(2)/M cell-arrest and microtubule destabilization. For chalcones, the results suggest an anti-proliferative activity. Also, results for combination-therapy potentiated the antitumor effect of doxorubicin and reduced cytotoxicity in MCF-10A cells. (C) 2018 Elsevier Masson SAS. All rights reserved.
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