First synthesis of N-[(aziridin-2-yl)methyl]benzimidazolequinone and analysis of toxicity towards normal and Fanconi anemia cells

被引:23
|
作者
O'Donovan, Liz [2 ]
Carty, Michael P. [1 ]
Aldabbagh, Fawaz [2 ]
机构
[1] Natl Univ Ireland, Dept Biochem, Sch Nat Sci, Galway, Ireland
[2] Natl Univ Ireland, Sch Chem, Galway, Ireland
基金
爱尔兰科学基金会;
关键词
D O I
10.1039/b814706j
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A diazole is N-substituted with 1-trityl-2-methylaziridine and demethylated and oxidised with NBS under acidic conditions to give a benzimidazolequinone; this novel anti-tumour agent is marginally more cytotoxic than mitomycin C (MMC) towards the normal human fibroblast cell line GM00637, while the MMC-hypersensitive human Fanconi anaemia (FA) cell line, PD20i, lacking the FANCD2 protein, is also hypersensitive to the benzimidazolequinone, with expression of FANCD2 protein decreasing sensitivity to both MMC and the benzimidazolequinone.
引用
收藏
页码:5592 / 5594
页数:3
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