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新型噻吩-2-甲酰基缩氨硫脲席夫碱铂(II)和钯(II)配合物及其抗病毒和细胞毒性活性。

Novel platinum(II) and palladium(II) complexes of thiosemicarbazones derived from 5-substitutedthiophene-2-carboxaldehydes and their antiviral and cytotoxic activities.

机构信息

Department of Chemistry, Faculty of Arts and Sciences, Gaziantep University, 27310 Gaziantep, Turkey.

出版信息

Eur J Med Chem. 2011 Nov;46(11):5616-24. doi: 10.1016/j.ejmech.2011.09.031. Epub 2011 Oct 1.

Abstract

A series of thiosemicarbazones and their platinum(II) and palladium(II) complexes have been synthesized. The chemical structures of ligands and their complexes were characterized by UV-Vis, IR, (1)H NMR, (13)C NMR, MS spectra, elemental analysis and TGA. The antiviral and cytotoxic activities of all compounds have been tested. Results of broad antiviral evaluation showed that none of the compounds evaluated endowed with anti-DNA or -RNA virus activity at subtoxic concentrations except for the palladium complex 1b. This compound exhibited slightly selective inhibition against cytomegalovirus. The platinum complex 4a exhibited the best cytostatic activities against human cervix carcinoma. Ligands 2, 4 and 5 showed cytostatic potential. The palladium complexes were in general less cytostatic than the corresponding platinum complexes or unliganded congeners.

摘要

一系列的缩氨基硫脲及其铂(II)和钯(II)配合物已经被合成。配体及其配合物的化学结构通过紫外可见光谱、红外光谱、(1)H NMR、(13)C NMR、质谱、元素分析和热重分析进行了表征。所有化合物的抗病毒和细胞毒性活性都已经进行了测试。广泛的抗病毒评估结果表明,在所测试的浓度下,除钯配合物 1b 外,没有一种化合物具有抗 DNA 或 RNA 病毒的活性。该化合物对巨细胞病毒表现出轻微的选择性抑制作用。铂配合物 4a 对人宫颈癌具有最好的细胞生长抑制活性。配体 2、4 和 5 显示出细胞生长抑制的潜力。钯配合物通常比相应的铂配合物或无配位同系物的细胞生长抑制活性低。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b21/7126824/8ae381a353e2/fx1_lrg.jpg

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