163883-05-4Relevant academic research and scientific papers
Polybenzofulvene derivatives bearing dynamic binding sites as potential anticancer drug delivery systems
Cappelli, Andrea,Grisci, Giorgio,Paolino, Marco,Razzano, Vincenzo,Giuliani, Germano,Donati, Alessandro,Bonechi, Claudia,Mendichi, Raniero,Boccia, Antonella Caterina,Licciardi, Mariano,Scialabba, Cinzia,Giammona, Gaetano,Vomero, Salvatore
, p. 361 - 374 (2015)
In order to obtain new advanced functional materials capable of recognizing drug molecules, the polybenzofulvene backbone of molecular brush poly-6-MOEG-9-TM-BF3k has been functionalized with a "synthetic dynamic receptor" composed of two 1-adamantylurea moieties linked together by means of a dipropyleneamino bridge as in Meijer's bis(adamantylurea) pincer (BAUP). This functional material, bearing synthetic receptors potentially capable of recognizing/loading and then delivering drug molecules, was used to prepare colloidal drug delivery systems (by means of soft interaction with BAUP) for delivering the model anti-cancer drug doxorubicin (DOXO). The resulting nanostructured drug delivery systems containing the physically loaded drug were characterized in terms of drug loading and release, dimensions and zeta potential, and in vitro cell activity and uptake on two different cell lines (i.e. the human bronchial epithelial 16HBE and the human colon cancer HCT116). On normal cells, free DOXO was found to be more cytotoxic than DOXO-loaded nanogels at the higher tested concentration and, only on cancer cells, DOXO-loaded nanogels show similar or slightly higher cytotoxicity values than free DOXO, suggesting potential advantages in the treatment of cancer. These results were supported by fluorescence microscopy studies, which suggested that DOXO-loaded nanogels provide an extracellular reservoir of the drug, which is gradually released and internalized within the cells.
Polyamine transport inhibitors
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Page/Page column 31, (2010/02/14)
The present invention describes the design, synthesis and therapeutic use of a variety of novel inhibitors of polyamine transport. The main feature of this class of transport inhibitors is to incorporate a linker or side chain that prevents the uptake of
Synthesis of spermidine and norspermidine dimers as high affinity polyamine transport inhibitors
Covassin, Laurence,Desjardins, Michel,Charest-Gaudreault, Rene,Audette, Marie,Bonneau, Marie-Josee,Poulin, Richard
, p. 1709 - 1714 (2007/10/03)
A series of novel spermidine and sym-norspermidine dimers was synthesized by crosslinking the polyamine backbones via alkylation of their secondary amino groups to butyl, trans-2-butenyl, 2-butynyl or pxylyl bridges. The resulting hexamines behaved as high-affinity antagonists of polyamine uptake, with a relative potency that was dependent on the geometry of the linker structure.
