Synthesis of N²-modified 7-methylguanosine 5'-monophosphates as nematode translation inhibitors.

Synthesis of N²-modified 7-methylguanosine 5'-monophosphates as nematode translation inhibitors.
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DOI:
10.1016/j.bmc.2012.05.078
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发表时间:
2012-08-01
影响因子:
3.5
通讯作者:
Jankowska-Anyszka, Marzena
Jankowska-Anyszka, Marzena
中科院分区:
医学3区
文献类型:
--
作者:
Piecyk, Karolina;Davis, Richard E.;Jankowska-Anyszka, Marzena

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Preparative scale synthesis of fourteen new N2-modified mononucleotide 5’ mRNA cap analogues was achieved. The key step involved use of an SNAr reaction with protected 2-fluoro inosine and various primary and secondary amines. The derivatives were tested in a parasitic nematode, Ascaris suum, cell-free system as translation inhibitors. The most effective compound with IC50 ~ 0.9 μM was a N2-p-metoxybenzyl-7-methylguanosine-5’-monophosphate 35.
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