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Title: | Anticancer activity of novel hybrid molecules containing 5-benzylidene thiazolidine-2,4-dione |
Authors: | Romagnoli, Romeo; Baraldi, Pier Giovanni; Salvador, Maria Kimatrai; Camacho, M. Encarnación; Bermejo, Jaime ![]() |
Keywords: | Apoptosis Structureeactivity relationship In vitro antiproliferative activity Caspases Thiazolidine-2,4-dione |
Issue Date: | May-2013 |
Publisher: | Elsevier |
Citation: | European Journal of Medicinal Chemistry 63: 544-557 (2013) |
Abstract: | Hybridization 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 |
URI: | http://hdl.handle.net/10261/178300 |
DOI: | 10.1016/j.ejmech.2013.02.030 |
Identifiers: | doi: 10.1016/j.ejmech.2013.02.030 issn: 0223-5234 e-issn: 1768-3254 |
Appears in Collections: | (IPNA) Artículos |
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