Publication Type Journal Article
Title Selenium-Containing Chrysin and Quercetin Derivatives: Attractive Scaffolds for Cancer Therapy
Authors Inês Sofia Lança Martins Catarina Sofia Romão Charneira Valentina Gandin João Ferreira da Silva Gonçalo C. Justino J. P. Telo Abel J. S. C. Vieira Cristina Marzano Alexandra Maria Moita Antunes
Groups BioMol
Journal JOURNAL OF MEDICINAL CHEMISTRY
Year 2015
Month May
Volume 58
Number 10
Pages 4250-4265
Abstract Selenium-containing chrysin (SeChry) and 3,7,3 ,4 -tetramethylquercetin (SePQue) derivatives were synthesized by a microwave-based methodology. In addition to their improvement in terms of DPPH Scavenging and potential GPx-like activities, when tested in a panel of cancer cell lines both selenium-derivatives revealed consistently to be more cytoxic when compared with their oxo and thioanalogues, evidencing the key role of selenocabonyl Moiety for these activities In particular, SeChry elicited a noteworthy cytotoxic activity with mean IC50 values 18- and 3-fold lower than those observed for chrysin and cisplatin, respectively. Additionally, these seleno-derivatives evidenced an ability to overcome cisplatin and multidrug resistance. Notably, a differential behavior toward malignant and nonmalignant cells Was observed for SeChry and SePQue, exhibiting higher selectivity indexes when compared with the chalcogen-derivatives and cisplatin. Our preliminary investigation on the mechanism of cytotoxicity of SeChry and SePQue in MCF-7 human mammary cancer cells demonstrated their capacity to efficiently suppress the clonal expansion along with their ability to hamper TrxR activity leading to apoptotic cell death.
DOI http://dx.doi.org/10.1021/acs.jmedchem.5b00230
ISBN
Publisher
Book Title
ISSN 0022-2623
EISSN 1520-4804
Conference Name
Bibtex ID ISI:000355495200010
Observations
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