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吖啶硫脲及其衍生物的研究进展：生物活性和细胞毒性。

A review on acridinylthioureas and its derivatives: biological and cytotoxic activity.

机构信息

Department of Biochemisty, Institute of Chemistry, P.J. Šafárik University Košice, Moyzesova 11, Košice, Slovak Republic.

Biomedical Research Center, University Hospital Hradec Kralove, Sokolovska 581, Hradec Kralove, Czech Republic.

出版信息

J Appl Toxicol. 2017 Oct;37(10):1132-1139. doi: 10.1002/jat.3464. Epub 2017 Mar 31.

DOI:10.1002/jat.3464
PMID:28370171
Abstract

Acridines possess two characteristics that have led many researchers to consider the agents interesting targets for future development as potential farmacophores: the planar acridine skeleton, which is able to intercalate into DNA, and the intense fluorescence of the agents. This review offers a study of the multifunctional character of acridines and the synthesis of novel acridine derivatives, with particular focus being placed on isothiocyanates and their congeners, e.g. thioureas, isothioureas, quaternary ammonium salts and platinum/gold conjugates. The review provides an overview of the structure, spectral properties, DNA binding and biological activity of acridinylthiourea congeners. These acridinylthiourea derivatives display significant cytotoxic activities against different types of cancer cell lines at micromolar concentrations. Copyright © 2017 John Wiley & Sons, Ltd.

摘要

吖啶具有两个特点，这使得许多研究人员认为该类化合物是未来发展的有前途的药物靶标：平面吖啶骨架，能够嵌入 DNA 中，以及该类化合物强烈的荧光。本综述研究了吖啶的多功能特性和新型吖啶衍生物的合成，特别关注异硫氰酸酯及其同系物，例如硫脲、异硫脲、季铵盐和铂/金缀合物。本综述概述了吖啶基硫脲同系物的结构、光谱性质、DNA 结合和生物活性。这些吖啶基硫脲衍生物在微摩尔浓度下对不同类型的癌细胞系显示出显著的细胞毒性活性。版权所有© 2017 年 John Wiley & Sons, Ltd.

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