Synthesis of N2-modified 7-METHYLGUANOSINE (cas 15313-37-8) 5′-monophosphates as nematode translation inhibitors
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Add time:08/06/2019 Source:sciencedirect.com
Preparative scale synthesis of 14 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 (cas 15313-37-8)-5′-monophosphate 35.
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