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大环 G-四链体配体。

Macrocyclic G-quadruplex ligands.

机构信息

Department of Physics and Chemistry, University of Southern Denmark, Odense M, Denmark.

出版信息

Curr Med Chem. 2010;17(29):3438-48. doi: 10.2174/092986710793176320.

DOI:10.2174/092986710793176320
PMID:20712562
Abstract

G-quadruplex stabilizing compounds have recently received increased interest due to their potential application as anticancer therapeutics. A significant number of structurally diverse G-quadruplex ligands have been developed. Some of the most potent and selective ligands currently known are macrocyclic structures which have been modeled after the natural product telomestatin or from porphyrin-based ligands discovered in the late 1990s. These two structural classes of G-quadruplex ligands are reviewed here with special attention to selectivity and structure-activity relationships, and with focus on the recent developments.

摘要

由于其在抗癌治疗方面的潜在应用,G-四链体稳定化合物最近受到了越来越多的关注。已经开发出了大量结构多样的 G-四链体配体。目前已知的一些最有效和选择性的配体是大环结构,这些结构是模仿天然产物端粒酶或 20 世纪 90 年代末发现的基于卟啉的配体而设计的。本文综述了这两类 G-四链体配体,特别关注其选择性和结构-活性关系,并重点介绍了最近的发展。

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