Synthesis of N²-modified 7-methylguanosine 5'-monophosphates as nematode translation inhibitors.
Bioorg Med Chem
; 20(15): 4781-9, 2012 Aug 01.
Article
in En
| MEDLINE
| ID: mdl-22748379
ABSTRACT
Preparative scale synthesis of 14 new N(2)-modified mononucleotide 5' mRNA cap analogues was achieved. The key step involved use of an S(N)Ar 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 IC(50) â¼0.9µM was a N(2)-p-metoxybenzyl-7-methylguanosine-5'-monophosphate 35.
Full text:
1
Database:
MEDLINE
Main subject:
RNA Cap Analogs
/
Protein Synthesis Inhibitors
/
Ascaris suum
/
Luciferases, Renilla
Limits:
Animals
Language:
En
Year:
2012
Type:
Article