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基于蒽环类药物的2-取代蒽醌的制备与评价

Preparation and evaluation of 2-substituted anthraquinones based on the anthracyclines.

作者信息

Bennett S, Sharples D, Brown J R

出版信息

J Med Chem. 1982 Apr;25(4):369-73. doi: 10.1021/jm00346a008.

DOI:10.1021/jm00346a008
PMID:7069715
Abstract

Anthraquinones substituted at the 2 position with a basic side chain were prepared, and their binding to DNA was evaluated. All compounds showed an intercalative mode of binding to DNA; 1,4-dihydroxy derivatives bound more strongly than 1-hydroxy or nonhydroxylated compounds. Greatest DNA-binding activity was found where there were five atoms between the anthraquinone ring and the basic nitrogen.

摘要

制备了在2位被碱性侧链取代的蒽醌，并评估了它们与DNA的结合情况。所有化合物均显示出与DNA的嵌入结合模式；1,4-二羟基衍生物的结合比1-羟基或未羟基化的化合物更强。在蒽醌环与碱性氮之间有五个原子的情况下，发现了最大的DNA结合活性。

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