申请人:Xiao Zejun
公开号:US20070004798A1
公开(公告)日:2007-01-04
Disclosed herein are novel platinum-based complexes possessing one nitrile substituent group (mononitrile) covalently-bonded to the platinum, one or more nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA and leaving groups (i.e., L
1
and L
2
) which can be hydrolyzed in vivo to active species, which can then form coordinate adducts with DNA or RNA at the Guanine or Adenine bases thereof. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as methods of treatment of various types of cancer by the administration of a pharmaceutically-effective dose of said novel platinum complexes.
本文披露了一种新型的基于铂的配合物,其具有一个腈基取代基(单腈基)与铂形成共价键结合,一个或多个氮供体配体能够与DNA或RNA中的碱基形成氢键,并且具有可以在体内水解为活性物种的离去基(即L1和L2),然后这些活性物种可以与DNA或RNA中的鸟嘌呤或腺嘌呤碱基形成配位加合物。本文还披露了合成所述铂配合物的反应方案,以及通过给予所述新型铂配合物的药效剂量来治疗各种类型的癌症的方法。