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基于 4-氨基-1,8-萘酰亚胺的 Troger 碱作为高亲和性 DNA 靶向荧光超分子支架。

4-Amino-1,8-naphthalimide-based Tröger's bases as high affinity DNA targeting fluorescent supramolecular scaffolds.

机构信息

School of Chemistry, Center for Synthesis and Chemical Biology, Trinity College Dublin, Dublin 2, Ireland.

出版信息

Org Lett. 2009 Sep 17;11(18):4040-3. doi: 10.1021/ol9013602.

DOI:10.1021/ol9013602
PMID:19681640
Abstract

The synthesis and photophysical and biological investigation of fluorescent 1,8-naphthalimide conjugated Troger's bases 1-3 are described. These structures bind strongly to DNA in competitive media at pH 7.4, with concomitant modulation in their fluorescence emission. These structures also undergo rapid cellular uptake, being localized within the nucleus within a few hours, and are cytotoxic against HL60 and (chronic myeloid leukemia) K562 cell lines.

摘要

本文描述了荧光 1,8-萘酰亚胺共轭 Troger's 碱 1-3 的合成及光物理和生物学研究。这些结构在 pH 7.4 的竞争介质中与 DNA 强烈结合，同时其荧光发射也随之调制。这些结构还能快速被细胞摄取，在数小时内定位于细胞核内，并对 HL60 和（慢性髓系白血病）K562 细胞系具有细胞毒性。

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