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N-杂环卡宾-胺型铂（II）配合物：开发铂类抗癌药物的新化学空间。

N-heterocyclic carbene-amine Pt(II) complexes, a new chemical space for the development of platinum-based anticancer drugs.

机构信息

Centre de Recherche de Gif, ICSN, CNRS UPR 2301, 1 Avenue de la Terrasse, 91198 Gif-sur-Yvette, France.

出版信息

J Med Chem. 2010 Mar 11;53(5):2146-54. doi: 10.1021/jm901693m.

DOI:10.1021/jm901693m
PMID:20148592
Abstract

N-Heterocyclic carbene (NHC) platinum complexes have been highlighted as a promising and original platform for building new cytotoxic drugs of the cisplatin series. Mixed NHC-amine Pt(II) complexes have been prepared via a facile and modular two step sequence leading to trans-configured square planar species. They have been characterized by spectroscopic methods and X-ray diffraction studies. Their efficiency against both cisplatin sensitive (CEM and H460) and resistant (A2780/DDP, CH1/DDP, and SK-OV-3) cell lines has been demonstrated by in vitro experiments.

摘要

N-杂环卡宾（NHC）铂配合物已被作为构建顺铂系列新型细胞毒药物的一个很有前途和新颖的平台而受到关注。通过简便且模块化的两步序列制备了混合 NHC-胺 Pt(II)配合物，得到反式构型的平面四方物种。通过光谱方法和 X 射线衍射研究对其进行了表征。通过体外实验证明了它们对顺铂敏感（CEM 和 H460）和耐药（A2780/DDP、CH1/DDP 和 SK-OV-3）细胞系的有效性。

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