Pb. Arimondo et al., Recognition and cleavage of DNA by rebeccamycin- or benzopyridoquinoxalineconjugated of triple helix-forming oligonucleotides, BIO MED CH, 8(4), 2000, pp. 777-784
Indolocarbazole and benzopyridoquinoxaline derivatives have been shown to h
ave anti-tumor activity and to stimulate DNA topoisomerase I-mediated cleav
age. Two indolocarbazole compounds (R-6 and R-95) and one benzopyridoquinox
aline derivative (BPQ(1256)) were covalently attached to the 3'-end of a 16
mer triple helix-forming oligonucleotide (TFO). These conjugates bind to DN
A with a higher affinity than the unsubstituted oligonucleotides. Furthermo
re, they induce topoisomerase I-mediated and tripler-directed DNA cleavage
in a sequence-specific manner. (C) 2000 Elsevier Science Ltd. All rights re
served.