发明名称 Monoimine ligand platinum analogs
摘要 Disclosed herein are novel platinum-based analogs with a single substituted imine ligand: R<SUB>7</SUB>RC-NR<SUB>8</SUB>, wherein the R<SUB>7</SUB>RC-NR<SUB>8 </SUB>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.
申请公布号 US7268244(B2) 申请公布日期 2007.09.11
申请号 US20060340806 申请日期 2006.01.26
申请人 BIONUMERIK PHARMACEUTICALS, INC. 发明人 HAUSHEER FREDERICK H.;XIAO ZEJUN;KOCHAT HARRY
分类号 C07F15/00;A61K31/28 主分类号 C07F15/00
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