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ACS Medicinal Chemistry Letters
K. A.; Otto, M. J.; Furman, P. A.; Stec, W. J.; Patterson, S. E.;
Supporting Information
Pankiewiez, K. W. Design, synthesis, and antiviral activity of 2'ꢀ
deoxyꢀ2'ꢀfluoroꢀ2'ꢀCꢀmethylcytidine, a potent inhibitor of hepatitis C
virus replication. J. Med. Chem. 2005, 48, 5504ꢀ5508.
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The Supporting Information is available free of charge on the
ACS Publications website.
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(12) Murakami, E.; Tolstykh, T.; Bao, H.; Niu, C.; Steuer, H. M.
M.; Bao, D.; Chang, W.; Espiritu, C.; Bansal, S.; Lam, A. M.; Otto,
M. J.; Sofia, M. J.; Furman, P. A. Mechanism of activation of PSIꢀ
7851 and its diastereoisomer PSIꢀ7977. J. Biol. Chem. 2010, 285,
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(13) Jonckers, T. H. M.; Lin, T.ꢀI.; Buyck, C.; LachauꢀDurand, S.;
Vandyck, K.; Van Hoof, S.; Vandekerckhove, L. A. M.; Hu, L.;
Berke, J. M.; Vijgen, L.; Dillen, L. L. A.; Cummings, M. D.; de Kock,
H.; Nilsson, M.; Sund, C.; Rydegård, C.; Samuelsson, B.; Rosenquist,
Å.; Fanning, G.; Van Emelen, K.; Simmen, K.; Raboisson, P. 2'ꢀ
Deoxyꢀ2'ꢀspirocyclopropylcytidine revisited: a new and selective
inhibitor of the hepatitis C virus NS5B polymerase. J. Med. Chem.
2010, 53, 8150ꢀ8160.
Full experimental details, in vitro antiviral activity and cytotoxiciꢀ
ty assay (PDF)
AUTHOR INFORMATION
Corresponding Author
* Eꢀmail: zheng_yin@nankai.edu.cn for Dr Zheng Yin.
shanglq@nankai.edu.cn for Dr Luqing Shang.
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Author Contributions
The manuscript was written through the contributions of all auꢀ
thors. All authors have given their approval to the final version of
the manuscript.
(14) Du, J.; Chun, B.ꢀK.; Mosley, R. T.; Bansal, S.; Bao, H.; Espirꢀ
itu, C.; Lam, A. M.; Murakami, E.; Niu, C.; Micolochick Steuer, H.
M.; Furman, P. A.; Sofia, M. J. Use of 2'ꢀspirocyclic ethers in HCV
nucleoside design. J. Med. Chem. 2013, 57, 1826ꢀ1835.
Funding Sources
This work was supported by the National Basic Research Program
of China (973 program, Grant No. 2013CB911104,
(15) Cui, H.ꢀK.; Qing, J.; Guo, Y.; Wang, Y.ꢀJ.; Cui, L.ꢀJ.; He, T.ꢀ
H.; Zhang, L.; Liu, L. Stapled peptideꢀbased membrane fusion inhibiꢀ
tors of hepatitis C virus. Bioorg. Med. Chem. 2013, 21, 3547ꢀ3554.
(16) Sofia, M. J.; Bao, D.; Chang, W.; Du, J.; Nagarathnam, D.;
Rachakonda, S.; Reddy, P. G.; Ross, B. S.; Wang, P.; Zhang, H.ꢀR.;
Bansal, S.; Espiritu, C.; Keilman, M.; Lam, A. M.; Steuer, H. M. M.;
Niu, C.; Otto, M. J.; Furman, P. A. Discovery of a βꢀDꢀ2'ꢀdeoxyꢀ2'ꢀαꢀ
fluoroꢀ2'ꢀβꢀCꢀmethyluridine nucleotide prodrug (PSIꢀ7977) for the
treatment of hepatitis C Virus. J. Med. Chem. 2010, 53, 7202ꢀ7218.
(17) Chou, T.ꢀF.; Baraniak, J.; Kaczmarek, R.; Zhou, X.; Cheng, J.;
Ghosh, B.; Wagner, C. R. Phosphoramidate pronucleotides: a comparꢀ
ison of the phosphoramidase substrate specificity of human and Eschꢀ
erichia coli histidine triad nucleotide binding proteins. Mol. Pharma-
ceutics 2007, 4, 208ꢀ217.
(18) Lima, C. D.; Klein, M. G.; Hendrickson, W. A. Structureꢀ
based analysis of catalysis and substrate definition in the HIT protein
family. Science 1997, 278, 286ꢀ290.
(19) Appleby, T. C.; Perry, J. K.; Murakami, E.; Barauskas, O.;
Feng, J.; Cho, A.; Fox, D., III; Wetmore, D. R.; McGrath, M. E.; Ray,
A. S.; Sofia, M. J.; Swaminathan, S.; Edwards, T. E. Structural basis
for RNA replication by the hepatitis C virus polymerase. Science
2015, 347, 771ꢀ775.
2013CB911100), the National Natural Science Foundation of
China (Grant No. 21202087, 31200586, 21572116), the Tianjin
Science and Technology Program (Grant No. 13JCYBJC24300,
13JCQNJC13100), and the "111" Project of the Ministry of Eduꢀ
cation of China (Project No. B06005).
Notes
The authors declare no competing financial interest.
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