Structure-Activity Relationships Among a New Class of Antiviral Heterosubstituted 2′,3′-Dideoxynucleoside Analogues

Tarek S. Mansour BioChem Therapeutic Inc., 275 Armand-Frappier Boulevard, Laval (Quebec), Canada, H7V 4A7

Haolun Jin BioChem Therapeutic Inc., 275 Armand-Frappier Boulevard, Laval (Quebec), Canada, H7V 4A7

Wei Wang BioChem Therapeutic Inc., 275 Armand-Frappier Boulevard, Laval (Quebec), Canada, H7V 4A7

Dilip M. Dixit BioChem Therapeutic Inc., 275 Armand-Frappier Boulevard, Laval (Quebec), Canada, H7V 4A7

Colleen A. Evans BioChem Therapeutic Inc., 275 Armand-Frappier Boulevard, Laval (Quebec), Canada, H7V 4A7

H. L. Allan Tse BioChem Therapeutic Inc., 275 Armand-Frappier Boulevard, Laval (Quebec), Canada, H7V 4A7

Bernard Belleau BioChem Therapeutic Inc., 275 Armand-Frappier Boulevard, Laval (Quebec), Canada, H7V 4A7

John W. Gillard BioChem Therapeutic Inc., 275 Armand-Frappier Boulevard, Laval (Quebec), Canada, H7V 4A7

Elizabeth Hooker Department of Virology, Glaxo Research and Development Ltd., Greenford Road, Greenford, Middlesex, United Kingdom, UB6 OHE

Claire Ashman Department of Virology, Glaxo Research and Development Ltd., Greenford Road, Greenford, Middlesex, United Kingdom, UB6 OHE

Nick Cammack Department of Virology, Glaxo Research and Development Ltd., Greenford Road, Greenford, Middlesex, United Kingdom, UB6 OHE

Horacio Salomon Lady Davis Institute - Jewish General Hospital, and McGill AIDS Centre, McGill University, Montreal, Quebec, Canada, H3T 1E2

Antonietta R. Belmonte Lady Davis Institute - Jewish General Hospital, and McGill AIDS Centre, McGill University, Montreal, Quebec, Canada, H3T 1E2

Mark A. Wainberg Lady Davis Institute - Jewish General Hospital, and McGill AIDS Centre, McGill University, Montreal, Quebec, Canada, H3T 1E2

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Abstract

3′-Oxa-4′-thiocytidine nucleoside analogues 14–17 were prepared from oxathiolanes 10 and 11, and evaluated for activity against HIV-1 and HBV in vitro. The nucleoside analogues were found to possess potent activities against HIV-1 in a panel of cell lines. Compound 16 is moderately active against HBV in 2.2.15 cells.

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Structure-Activity Relationships Among a New Class of Antiviral Heterosubstituted 2′,3′-Dideoxynucleoside Analogues

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Structure-Activity Relationships Among a New Class of Antiviral Heterosubstituted 2′,3′-Dideoxynucleoside Analogues

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