Biological Activity
psi-6206 (as known as ro-2433 or gs-331007), β-d-2’-deoxy-2’-fluoro-2’-c-methyluridine, is the deaminated derivative of psi-6130, β-d-2’-deoxy-2’-fluoro-2’-c-methylcytidine, which is a potent inhibitor of hepatitis c virus (hcv) replication in the subgenomic hcv reolicon system. psi-6206, itself, does not shown any inhibitory activity towards hcv replication in the hcv subgenomic replicon system. however, the its triphosphate form, ro2433-tp, is a potent inhibitor of rna synthesis by hcv polymerase, which inhibits both the rna sysnthesis activity of hcv replicase (ic50 = 1.19 um) and the rna synthesis activity of the recombinant hcv con1 ns58 on a heteropolymeric rna template derived from the 3’-end of the negative strand of the hcv genome (ic50 = 0.52 um and ki = 0.141 um).han ma, wen-rong jiang, nicole robledo, vincent leveque, samir ali, teresa lara-jamie, mohammad masjedizadeh, david b. smith, nick cammack, klaus klumpp, and julian symons. characterization of the metabolic ctivation of hepatitis c virus nucleoside inhibitor β-d-2’-deoxy-2’-fluoro-2’-c-methylcytidine (psi-6130) and identification of a novel active 5’-triphosphate species. the journal of biological chemistry 2007; 282(41): 29812-29820
