Among the challenges precluding the widespread use of BNCT has been the difficulty in achieving selective delivery of large quantities of boron to malignant cells. In an attempt to address this issue we have recently developed an effective strategy to synthesize a new family of boronate dporphyrazines to be delivered through the membrane of cancerous tissues as such or with th help of liposomes. Herein we describe the synthesis and the basic physico-chemical properties of neutral octa-closo-carboranyl-alkylthio-porphyrazines as well as of their water -soluble counterparts obtained by mild boronation of the closo-polyhedra. Preliminary studies indicate that these compounds show negligible cell toxicity and, compared with BPA, good cellular uptake. This encourages further studies for their evaluation as potential BNCT sensitizers.

Carboranylporphyrazines: Synthetic Aspects and Molecular Properties

RICCIARDI, Giampaolo
2008

Abstract

Among the challenges precluding the widespread use of BNCT has been the difficulty in achieving selective delivery of large quantities of boron to malignant cells. In an attempt to address this issue we have recently developed an effective strategy to synthesize a new family of boronate dporphyrazines to be delivered through the membrane of cancerous tissues as such or with th help of liposomes. Herein we describe the synthesis and the basic physico-chemical properties of neutral octa-closo-carboranyl-alkylthio-porphyrazines as well as of their water -soluble counterparts obtained by mild boronation of the closo-polyhedra. Preliminary studies indicate that these compounds show negligible cell toxicity and, compared with BPA, good cellular uptake. This encourages further studies for their evaluation as potential BNCT sensitizers.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11563/13132
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