Synthesis, cellular uptake and animal toxicity of a tetra(carboranylphenyl)-tetrabenzoporphyrin

被引：56

作者：

Gottumukkala, V

Ongayi, O

Baker, DG

Lomax, LG

Vicente, MGH ^{[1
]}

机构：

[1] Louisiana State Univ, Dept Chem, Baton Rouge, LA 70803 USA

[2] Sch Vet Med, Dept Pathobiol Sci, Baton Rouge, LA 70803 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 06期

关键词：

BNCT; PDT; nido-carborane; tetrabenzoporphyrin;

D O I：

10.1016/j.bmc.2005.10.037

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：1871 / 1879

页数：9

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[1] Boron neutron capture therapy of cancer: Current status and future prospects [J].