Propargylated Purine Deoxynucleosides: New Tools for Fluorescence Imaging Strategies

被引：9

作者：

Venkatesham, Akkaladevi ^{[1
]}

Pillalamarri, Sambasiva Rao ^{[1
]}

De Wit, Flore ^{[2
]}

Lescrinier, Eveline ^{[1
]}

Debyser, Zeger ^{[2
]}

Van Aerschot, Arthur ^{[1
]}

机构：

[1] Katholieke Univ Leuven, Rega Inst Med Res, Dept Pharmaceut & Pharmacol Sci, Med Chem, Herestr 49, B-3000 Leuven, Belgium

[2] Katholieke Univ Leuven, Dept Pharmaceut & Pharmacol Sci, Lab Mol Virol & Gene Therapy, Kapucijnenvoer 33, B-3000 Leuven, Belgium

来源：

MOLECULES | 2019年 / 24卷 / 03期

关键词：

click reaction; propargylated nucleosides; imaging; DNA visualization; fluorophores; ethynyl-2 '-deoxyuridine (EdU); HIV toxicity; Mitsunobu reaction; NUCLEAR-ORGANIZATION; DNA; PHOSPHORAMIDITES; VISUALIZATION; REPLICATION; CLUSTERS;

D O I：

10.3390/molecules24030468

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

In vivo imaging of biological processes is an important asset of modern cell biology. Selectively reacting fluorophores herein are an important tool and click chemistry reactions take a large share in these events. 5-Ethynyl-2'-deoxyuridine (EdU) is well known for visualizing DNA replication, but does not show any selectivity for incorporation into DNA. Striving for specific visualization of virus replication, in particular HIV replication, a series of propargylated purine deoxynucleosides were prepared aiming for selective incorporation by HIV reverse transcriptase (RT). We here report on the synthesis and preliminary biological effects (cellular toxicity, HIV inhibitory effects, and feasibility of the click reaction) of these nucleoside analogues.

引用

页数：16

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