Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 14, Issue 6, Pages 1871-1879Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2005.10.037
Keywords
BNCT; PDT; nido-carborane; tetrabenzoporphyrin
Funding
- NCI NIH HHS [CA098902] Funding Source: Medline
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A water-soluble nido-carboranyl-tetrabenzoporphyrin has been synthesized in 43% overall yield, by condensation of butanopyrrole with a carboranylbenzaldehyde, followed by metal insertion, oxidation, demetallation and deboronation reactions. This Compound accumulated within human glioblastoma T98G cells to a significant higher extent than a structurally related nido-carboranylporphyrin, and localized preferentially in the cell lysosomes. Animal toxicity studies using male and female BALB/c mice revealed that both compounds are non-toxic even at a dose of 160 mg/kg, administered intraperitoneally as a single injection at a concentration of 4 mg/mL. It is concluded that the tetra(carboranylphenyl)-tetrabenzoporphyrin is a promising new sensitizer for the treatment of malignant tumors. (c) 2005 Elsevier Ltd. All rights reserved.
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