Arimondo P B, Moreau P, Boutorine A, Bailly C, Prudhomme M, Sun J S, Garestier T, Hélène C
Laboratoire de Biophysique, UMR 8646 CNRS-Muséum National d'Histoire Naturelle, INSERM U201, Paris, France.
Bioorg Med Chem. 2000 Apr;8(4):777-84. doi: 10.1016/s0968-0896(00)00012-2.
Indolocarbazole and benzopyridoquinoxaline derivatives have been shown to have anti-tumor activity and to stimulate DNA topoisomerase I-mediated cleavage. Two indolocarbazole compounds (R-6 and R-95) and one benzopyridoquinoxaline derivative (BPQ(1256)) were covalently attached to the 3'-end of a 16mer triple helix-forming oligonucleotide (TFO). These conjugates bind to DNA with a higher affinity than the unsubstituted oligonucleotides. Furthermore, they induce topoisomerase I-mediated and triplex-directed DNA cleavage in a sequence-specific manner.