4-Amino-1,8-naphthalimide-Based Troger's Bases As High Affinity DNA Targeting Fluorescent Supramolecular Scaffolds

4-Amino-1,8-naphthalimide-Based Troger's Bases As High Affinity DNA Targeting Fluorescent Supramolecular Scaffolds
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DOI:
10.1021/ol9013602
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发表时间:
2009-09-17
期刊:
影响因子:
5.2
通讯作者:
Gunnlaugsson, Thorfinnur
Gunnlaugsson, Thorfinnur
中科院分区:
化学1区
文献类型:
--
作者:
Veale, Emma B.;Frimannsson, Daniel O.;Gunnlaugsson, Thorfinnur

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本文报道了荧光1,8-萘酰亚胺共轭Troger碱1-3的合成及其生物和物理性质的研究。这些结构在pH 7.4的竞争性介质中与DNA强烈结合,伴随着它们的荧光发射的调制。这些结构还经历快速的细胞摄取,在几小时内定位在细胞核内,并且对HL 60和(慢性髓性白血病)K562细胞系具有细胞毒性。
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.