The influence of the aziridinyl substituent of benzimidazoles and benzimidazolequinones on toxicity towards normal and Fanconi anaemia cells

European Journal of Medicinal Chemistry
Karen FaheyFawaz Aldabbagh

Abstract

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.

References

Jul 21, 2004·Il Farmaco·Laura GarutiSilvana Hrelia
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Feb 24, 2006·Blood·Toshiyasu Taniguchi, Alan D D'Andrea
May 17, 2007·Mini Reviews in Medicinal Chemistry·Laura GarutiDaniela Pizzirani

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Citations

Oct 30, 2014·Chemical Biology & Drug Design·Rangappa S KeriBhari Mallanna Nagaraja
Apr 3, 2021·Bioorganic Chemistry·Claudia López-LiraEugenio Uriarte
Jun 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Martin SweeneyFawaz Aldabbagh

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