Publication date: Available online 24 October 2015
Source:Bioorganic & Medicinal Chemistry
Author(s): Francis Giraud, Marion Bourhis, Edris Ebrahimi, Lars Herfindal, Romy Roy Choudhury, Ronja Bjørnstad, Stein Ove Døskeland, Fabrice Anizon, Pascale Moreau
The synthesis of new indolopyrrolobenzodiazepine derivatives is described. Six compounds were selected for evaluation of cytotoxicity towards acute myeloid leukemia (AML) cells and normal fibroblasts. One compound (29) showed selective AML cell death induction. Its action was only partly overcome by knock-down of p53 or Bcl-2 overexpression, suggesting a strong activation of intrinsic apoptotic pathways.
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