Synthesis, DNA binding and biological activity of oxazolopyridocarbazole-netropsin hybrid molecules

Article abstract of DOI:10.1016/0223-5234(91)90143-B

A series of bifunctional molecules have been synthesized which result from the combination of a DNA sequence-specific ligand (netropsin) coupled to an intercalator moiety (OPC).The binding constants to double-stranded polynucleotides as well as the cytostatic activity against both murine and human tumor cell lines and the in vitro activity against a range of DNA and RNA viruses (including human immunodeficiency virus) have been determined for these novel molecules.All of them retain the DNA binding affinity of netropsin but with a notable decrease of A-T sequence selectivity.They did not show in vitro antiviral activity.On the other hand these compounds demonstrated enhanced cytostatic activity against both human and murine tumor cell lines.