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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 Encarnacion
Balzarini, Jan
Bermejo, Jaime
Estévez, Francisco #
Issue Date: Mar-2013
Series Title: European Journal of Medicinal Chemistry vol:63 pages:544-557
Article number: S0223-5234(13)00137-2
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.
URI: 
ISSN: 0223-5234
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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