Studies on Enzyme-Cleavable Dialkoxymethyl-cyclo Saligenyl-2′, 3′-dideoxy-2′, 3′-didehydrothymidine Monophosphates

N Gisch, J Balzarini, C Meier

Index: Gisch, Nicolas; Balzarini, Jan; Meier, Chris Journal of Medicinal Chemistry, 2008 , vol. 51, # 21 p. 6752 - 6760

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Citation Number: 22

Abstract

Recently we reported on conceptually new enzymatically activated cyclo Sal-pronucleotides. Now, we developed this concept further with new compounds of this type. The basic idea is fast intracellular cleavage of a functionalized group at the cyclo Sal residue that results in a rapid delivery of the nucleotide and thus an intracellular enrichment of the nucleotide. The introduction of a higher alkylated acylal group, the di-iso-butyryloxymethyl group, to the ...