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Synthesis and biological evaluation of a novel β-D-2'-deoxy-2'-α-fluoro-2'-β-C-(fluoromethyl)uridine phosphoramidate prodrug for the treatment of hepatitis C virus infection. 2018
Ertong Li, and
Yafeng Wang, and
Wenquan Yu, and
Zhigang Lv, and
Youmei Peng, and
Bingjie Liu, and
Shiliang Li, and
Wenzhe Ho, and
Qingduan Wang, and
Honglin Li, and
Junbiao Chang
College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001, China.
A novel β-D-2'-deoxy-2'-α-fluoro-2'-β-C-(fluoromethyl)uridine phosphoramidate prodrug (1) has been synthesized. This compound exhibits submicromolar-level antiviral activity in vitro against HCV genotypes 1b, 1a, 2a, and S282T replicons (EC50 = 0.18-1.13 μM) with low cytotoxicity (CC50 > 1000 μM). Administered orally, prodrug 1 is well tolerated at doses of up to 4 g/kg in mice, and produces a high level of the corresponding triphosphate in rat liver.
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