Search

Your search keyword '"Chun, Byoung-Kwon"' showing total 1 results
Start Over Author "Chun, Byoung-Kwon" Topic antiviral Topic antiviral agents
1 results on '"Chun, Byoung-Kwon"'

1. 2′-Deoxy-2′-α-fluoro-2′-β-C-methyl 3′,5′-cyclic phosphate nucleotide prodrug analogs as inhibitors of HCV NS5B polymerase: Discovery of PSI-352938

Author

Reddy, P. Ganapati, Bao, Donghui, Chang, Wonsuk, Chun, Byoung-Kwon, Du, Jinfa, Nagarathnam, Dhanapalan, Rachakonda, Suguna, Ross, Bruce S., Zhang, Hai-Ren, Bansal, Shalini, Espiritu, Christine L., Keilman, Meg, Lam, Angela M., Niu, Congrong, Steuer, Holly Micolochick, Furman, Phillip A., Otto, Michael J., and Sofia, Michael J.

Subjects
*NUCLEOTIDES, *PHOSPHATES, *PRODRUGS, *HEPATITIS C virus, *BIOLOGICAL assay, *LABORATORY rats, *DRUG administration, *ANTIVIRAL agents, *ENZYME inhibitors
Abstract

Abstract: A series of novel 2′-deoxy-2′-α-fluoro-2′-β-C-methyl 3′,5′-cyclic phosphate nucleotide prodrug analogs were synthesized and evaluated for their in vitro anti-HCV activity and safety. These prodrugs demonstrated a 10–100-fold greater potency than the parent nucleoside in a cell-based replicon assay due to higher cellular triphosphate levels. Our structure–activity relationship (SAR) studies provided compounds that gave high levels of active triphosphate in rat liver when administered orally to rats. These studies ultimately led to the selection of the clinical development candidate 24a (PSI-352938). [ABSTRACT FROM AUTHOR]

Published
2010
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results