期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 5, 页码 1873-1879出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.01.026
关键词
Aziridine; Bioreductive; Cytotoxicity; Mitomycin C; Quinones
资金
- Science Foundation Ireland [07/RFP/CHEF227]
- National Development Plan
- Health Research Board
- Science Foundation Ireland (SFI) [07/RFP/CHEF227] Funding Source: Science Foundation Ireland (SFI)
Aziridinyl substituted benzimidazolequinones are more toxic than methoxy analogues towards normal human fibroblast cells (GM00637). The aziridinyl substituent is required for hypersensitive killing of Fanconi anaemia (FA) cells (PD20i) deficient in FANCD2. Despite lacking quinone functionality, 4,7-dimethoxy-N-[(aziridin-2-yl)methyl]benzimidazole also induces hypersensitivity from FA cells, similar to their response towards mitomycin C. Expression of FANCD2 (in PD20:RV) corrects FA cell hypersensitivity supporting cellular response via the FANC pathway. (C) 2010 Elsevier Masson SAS. All rights reserved.
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