Cytotoxicity, cellular localisation and biomolecular interaction of non-covalent metallo-intercalators with appended sex hormonesteroid vectors

Abstract

A range of terpyridine platinum(II) metallo-intercalators with bioactive steroids attached has been created with the aim of localizing cytotoxic drugs. Complexes where the steroid does not interfere with access to the terpyridine are shown to retain potent cytotoxicity and show certain selectivity towards their natural receptors. Because the intercalation of the terpyridine moiety between the bases of the DNA is the origin of the biological activity, a dramatic decrease of the activity is observed when the access to the terpyridine unit is hindered by the steroidal unit.