Synthesis and characterization of copper(II) complexes of 4-alkyl/aryl-1,2-naphthoquinones thiosemicarbazones derivatives as potent DNA cleaving agents
Synthesis and characterization of copper(II) complexes of 4-alkyl/aryl-1,2-naphthoquinones thiosemicarbazones derivatives as potent DNA cleaving agents
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DOI：
10.1016/j.ica.2004.12.042
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发表时间：
2005-03-30
影响因子：
2.8
通讯作者：
Powell, AK
中科院分区：
文献类型：
--
作者：
Afrasiabi, Z;Sinn, E;Powell, AK
制备了一些烷基/芳基1,2萘醌硫代氨基脲铜配合物并对其进行了表征。其中一个游离配体4-吡咯烷-1-基-[1,2]萘醌硫代氨基脲(5)的晶体结构表明其结晶为“E”构象，这得到了核磁共振数据的支持。评价了配体和铜配合物在有氧条件下对环状双链质粒pBR322的DNA切割活性。在这些配体中，化合物8在H2O2氧化剂的存在下几乎可以定量转化为线性化的DNA。所有铜缀合物与DNA的相互作用更明显，而化合物3和7在氧化剂的存在下能够产生线性化的DNA。(c) 2005 Elsevier B.V.版权所有
Copper (II) complexes of some alkyl/aryl-1,2 naphthoquinones thiosemicarbazone have been prepared and characterized. The crystal structure determined for one of the free ligands viz. 4-Pyrrolidine-1-yl-[1, 2] naphthaquinone thiosemicarbazone (5) indicates it to crystallize in the "E" conformation which is supported by the NMR data. The ligands and copper complexes were evaluated for their DNA cleaving activities in case of circular double stranded plasmid DNA pBR322 under aerobic conditions. Amongst the ligands, compound 8 shows almost quantitative conversion to the linearized DNA in presence of H2O2 oxidant. All copper conjugates show more pronounced interaction with DNA while compounds 3 and 7 are able to yield linearized DNA in presence of the oxidant. (c) 2005 Elsevier B.V. All rights reserved.