| 摘要 |
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 dono r 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 o r other nucleophiles, which is thought to form active species in vivo, and the n, form cross-linked complexes between nucleic acid strands, principally betwee n purines in DNA (or RNA), i.e., at the Guanine or Adenine bases, thereof. The se platinum analogs may also be more easily transported into tumor cells, due t o their increased lipophilicity and are likely to be useful as anti-neoplastic agents, and in modulating or interfering with the synthesis or replication o r 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.
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