Disclosed herein are novel
platinum-based analogs with a single substituted
imine ligand: R7RC═NR8, wherein the R7RC═NR8 functional group is covalently bonded to the
platinum through
nitrogen. The analogs also have
nitrogen donor ligands capable of forming
hydrogen bonds with the bases in
DNA or
RNA, and one or more leaving groups which can be displaced by water,
hydroxide ions or other nucleophiles, which is thought to form active species
in vivo, and then, form cross-linked complexes between
nucleic acid strands, principally between purines in
DNA (or
RNA), i.e., at the
Guanine or Adenine bases, thereof. These
platinum analogs may also be more easily transported into
tumor cells, due to their increased
lipophilicity and are likely to be useful as anti-neoplastic agents, and in modulating or interfering with the synthesis or replication or transcription of
DNA or translation or function of
RNA in vitro or
in vivo, as they are potentially capable of forming a platinum coordinate complex with a intact or nascent DNA or RNA and thereby interfering with
cellular synthesis, transcription or replication of
nucleic acid polynucleotides.