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Title

Anticancer activity of novel hybrid molecules containing 5-benzylidene thiazolidine-2,4-dione

AuthorsRomagnoli, Romeo; Baraldi, Pier Giovanni; Salvador, Maria Kimatrai; Camacho, M. Encarnación; Bermejo, Jaime ; Estévez, Francisco
KeywordsApoptosis
Structureeactivity relationship
In vitro antiproliferative activity
Caspases
Thiazolidine-2,4-dione
Issue DateMay-2013
PublisherElsevier
CitationEuropean Journal of Medicinal Chemistry 63: 544-557 (2013)
AbstractHybridization of two different bioactive molecules with different mechanism of action is one of the methods that are being adopted to treat cancer. Molecules bearing a thiazolidine-2,4-dione scaffold have been recognized as antineoplastic agents with a broad spectrum of activity against many cancer cell lines. In this manuscript we have described the synthesis and biological evaluation of two series of N-3-substituted-5-arylidene thiazolidine-2,4-diones, bearing the α-bromoacryloylamido moiety at the para- or meta-position on the phenyl of the arylidene portion. We have observed that selected compounds 5a, 5c and 5g suppress proliferation of human myeloid leukaemia HL-60 and U937 cells by triggering morphological changes and internucleosomal DNA fragmentation, which are well-known features of apoptosis. Finally, our results indicated that the investigated compounds induced apoptotic cell death through a mechanism that involved activation of multiple caspases and was also associated with the release of cytochrome c from the mitochondria.
Publisher version (URL)https://doi.org/10.1016/j.ejmech.2013.02.030
URIhttp://hdl.handle.net/10261/178300
Identifiersdoi: 10.1016/j.ejmech.2013.02.030
issn: 0223-5234
e-issn: 1768-3254
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