REVIEW PSI-6206 is a selective HCV RNA polymerase inhibitor. Target: HCV. PSI-6206 is the unphosphorylated parent compound of triphosphate analog PSI-7409, which is a potent inhibitor of the HCV NS5B RNA dependent RNA polymerase. The monophosphate form of PSI-6206 was shown to be metabolized in primary human hepatocytes to its triphosphate analog PSI-7409. Furthermore, the phosphoramidate prodrug of PSI-6206 monophosphate, PSI-7851, was developed. Alternatively, PSI-6130, an aminated analog of PSI-6206 monophosphate, was also developed. PSI-7409, the triphosphate of PSI-6206 inhibits wild-type and S282T HCV RdRp with Ki values of 0.42 and 22 uM, respectively. PSI-7851, the phosphoramidate of PSI-6206 monophosphate, showed an EC50 value of 1.62 uM for inhibiting HCV RNA replication.
REFERENCES
[1]
Ma H, Jiang WR, Robledo N, Leveque V, Ali S, Lara-Jaime T, Masjedizadeh M, Smith DB, Cammack N, Klumpp K, Symons J. Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. J Biol Chem. 2007 Oct 12;282(41):29812-20.
[2]
Murakami E, Niu C, Bao H, Micolochick Steuer HM, Whitaker T, Nachman T, Sofia MA, Wang P, Otto MJ, Furman PA. The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. Agents Chemother. 2008 Feb;52(2):458-64.
[3]
Murakami E, Niu C, Bao H, Micolochick Steuer HM, Whitaker T, Nachman T, Sofia MA, Wang P, Otto MJ, Furman PA. The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. Agents Chemother. 2008 Feb;52(2):458-64.
[4]
Design, Synthesis, and Antiviral Activity of 2'-Deoxy-2'-fluoro-2'-C-methyl-cytidine, a Potent Inhibitor of Hepatitis C Virus Replication By Clark, Jeremy L.; Hollecker, Laurent; Mason, J. Christian; Stuyver, Lieven J.; Tharnish, Phillip M.; Lostia, Stefa J. Med. Chem., 2005, 48 (17), pp 5504-5508.
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