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Novel substituted pyrimidines as HCV replication (replicase) inhibitors. 2012
Cecil D Kwong, and
Jeremy L Clark, and
Anita T Fowler, and
Feng Geng, and
Hollis S Kezar, and
Abhijit Roychowdhury, and
Robert C Reynolds, and
Joseph A Maddry, and
Subramaniam Ananthan, and
John A Secrist, and
Neng-Yang Shih, and
John J Piwinski, and
Cheng Li, and
Boris Feld, and
Hsueh-Cheng Huang, and
Xiao Tong, and
F George Njoroge, and
Ashok Arasappan
Southern Research Institute, Birmingham, AL 35205, USA. kwong@southernresearch.org
Compound 1 was identified as a HCV replication inhibitor from screening/early SAR triage. Potency improvement was achieved via modulation of substituent on the 5-azo linkage. Due to potential toxicological concern, the 5-azo linkage was replaced with 5-alkenyl or 5-alkynyl moiety. Analogs containing the 5-alkynyl linkage were found to be potent inhibitors of HCV replication. Further evaluation identified compounds 53 and 63 with good overall profile, in terms of replicon potency, selectivity and in vivo characteristics. Initial target engagement studies suggest that these novel carbanucleoside-like derivatives may inhibit the HCV replication complex (replicase).
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Anita T Fowler, and
Feng Geng, and
Hollis S Kezar, and
Abhijit Roychowdhury, and
Robert C Reynolds, and
Joseph A Maddry, and
Subramaniam Ananthan, and
John A Secrist, and
Neng-Yang Shih, and
John J Piwinski, and
Cheng Li, and
Boris Feld, and
Hsueh-Cheng Huang, and
Xiao Tong, and
F George Njoroge, and
Ashok Arasappan
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Feng Geng, and
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Joseph A Maddry, and
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Joseph A Maddry, and
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Cheng Li, and
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Hsueh-Cheng Huang, and
Xiao Tong, and
F George Njoroge, and
Ashok Arasappan
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Bioorganic & medicinal chemistry letters,
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Jeremy L Clark, and
Anita T Fowler, and
Feng Geng, and
Hollis S Kezar, and
Abhijit Roychowdhury, and
Robert C Reynolds, and
Joseph A Maddry, and
Subramaniam Ananthan, and
John A Secrist, and
Neng-Yang Shih, and
John J Piwinski, and
Cheng Li, and
Boris Feld, and
Hsueh-Cheng Huang, and
Xiao Tong, and
F George Njoroge, and
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Feng Geng, and
Hollis S Kezar, and
Abhijit Roychowdhury, and
Robert C Reynolds, and
Joseph A Maddry, and
Subramaniam Ananthan, and
John A Secrist, and
Neng-Yang Shih, and
John J Piwinski, and
Cheng Li, and
Boris Feld, and
Hsueh-Cheng Huang, and
Xiao Tong, and
F George Njoroge, and
Ashok Arasappan
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Feng Geng, and
Hollis S Kezar, and
Abhijit Roychowdhury, and
Robert C Reynolds, and
Joseph A Maddry, and
Subramaniam Ananthan, and
John A Secrist, and
Neng-Yang Shih, and
John J Piwinski, and
Cheng Li, and
Boris Feld, and
Hsueh-Cheng Huang, and
Xiao Tong, and
F George Njoroge, and
Ashok Arasappan
May 2017,
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Feng Geng, and
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Joseph A Maddry, and
Subramaniam Ananthan, and
John A Secrist, and
Neng-Yang Shih, and
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Cheng Li, and
Boris Feld, and
Hsueh-Cheng Huang, and
Xiao Tong, and
F George Njoroge, and
Ashok Arasappan
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ACS medicinal chemistry letters,
Cecil D Kwong, and
Jeremy L Clark, and
Anita T Fowler, and
Feng Geng, and
Hollis S Kezar, and
Abhijit Roychowdhury, and
Robert C Reynolds, and
Joseph A Maddry, and
Subramaniam Ananthan, and
John A Secrist, and
Neng-Yang Shih, and
John J Piwinski, and
Cheng Li, and
Boris Feld, and
Hsueh-Cheng Huang, and
Xiao Tong, and
F George Njoroge, and
Ashok Arasappan
October 2013,
Bioorganic & medicinal chemistry letters,
Cecil D Kwong, and
Jeremy L Clark, and
Anita T Fowler, and
Feng Geng, and
Hollis S Kezar, and
Abhijit Roychowdhury, and
Robert C Reynolds, and
Joseph A Maddry, and
Subramaniam Ananthan, and
John A Secrist, and
Neng-Yang Shih, and
John J Piwinski, and
Cheng Li, and
Boris Feld, and
Hsueh-Cheng Huang, and
Xiao Tong, and
F George Njoroge, and
Ashok Arasappan
August 1973,
Archiv der Pharmazie,
Cecil D Kwong, and
Jeremy L Clark, and
Anita T Fowler, and
Feng Geng, and
Hollis S Kezar, and
Abhijit Roychowdhury, and
Robert C Reynolds, and
Joseph A Maddry, and
Subramaniam Ananthan, and
John A Secrist, and
Neng-Yang Shih, and
John J Piwinski, and
Cheng Li, and
Boris Feld, and
Hsueh-Cheng Huang, and
Xiao Tong, and
F George Njoroge, and
Ashok Arasappan
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