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新型多核铂抗肿瘤配合物的设计:基于联吡啶胺和1,3,5-三亚甲基苯的多齿配体体系

Toward the design of novel polynuclear platinum antitumor complexes: a polydentate ligand system based on dipyridylamine and 1,3,5-trimethylenebenzene.

作者信息

Tu Chao, Lin Jun, Shao Ying, Guo Zijian

机构信息

State Key Laboratory of Coordination Chemistry, Coordination Chemistry Institute, Nanjing University, 210093 Nanjing, P. R. China.

出版信息

Inorg Chem. 2003 Sep 22;42(19):5795-7. doi: 10.1021/ic034604q.

DOI:10.1021/ic034604q
PMID:12971744
Abstract

A novel hexadentate ligand, N,N,N',N',N",N"-hexa(2-pyridyl)-1,3,5-tris(aminomethyl)benzene (L), was designed and synthesized. The X-ray structure analysis reveals that the three dipyridylamine (DPA) groups of L are almost perpendicular to the central trimethylenebenzene, and two of them are spacially close to each other while the third one is further apart. The trinuclear Pt(II) complexes [Pt(3)LCl(6)] (1) and [Pt(3)L(CBDCA)(3)] (2) (where CBDCA represents cyclobutane dicarboxylic acid) were prepared and fully characterized by IR, NMR, and ESMS spectroscopy. A mononuclear complex, [PtL(CBDCA)] (3), was also prepared and structurally characterized, which suggests that controlled formation of mono-, di-, and trinuclear complexes with L is possible. Spectroscopic data showed that complexes 2 and 3 are able to bind to calf thymus DNA and their CBDCA group can be readily replaced by thiourea.

摘要

设计并合成了一种新型六齿配体N,N,N',N',N",N"-六(2-吡啶基)-1,3,5-三(氨甲基)苯(L)。X射线结构分析表明,L的三个二吡啶胺(DPA)基团几乎垂直于中心三亚甲基苯,其中两个在空间上彼此靠近,而第三个则相距较远。制备了三核铂(II)配合物Pt(3)LCl(6)和Pt(3)L(CBDCA)(3)(其中CBDCA代表环丁烷二羧酸),并通过红外光谱、核磁共振光谱和电喷雾质谱对其进行了全面表征。还制备了单核配合物PtL(CBDCA)并对其结构进行了表征,这表明与L可控形成单核、双核和三核配合物是可能的。光谱数据表明,配合物2和3能够与小牛胸腺DNA结合,并且它们的CBDCA基团可以很容易地被硫脲取代。

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