Please use this identifier to cite or link to this item: http://hdl.handle.net/10553/50548
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. Encarnacion
Balzarini, Jan
Bermejo, Jaime
Estévez, Francisco 
UNESCO Clasification: 32 Ciencias médicas
320713 Oncología
Keywords: Human Leukemia-Cells
Cytochrome-C
Cancer Cells
Caspases
Death, et al
Issue Date: 2013
Project: Evaluación de Potenciales Compuestos Antileucémicos. 
Journal: European Journal of Medicinal Chemistry 
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 alpha-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.
URI: http://hdl.handle.net/10553/50548
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2013.02.030
Source: European Journal of Medicinal Chemistry[ISSN 0223-5234],v. 63, p. 544-557
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