BMS-200475, a novel carbocyclic 2′-deoxyguanosine analog with potent and selective anti-hepatitis B virus activity in vitro
| Autor: | G. A. Jacobs, S. Innaimo, William A. Slusarchyk, O. Kocy, J.E. Sundeen, Robert Zahler, Alain Martel, M. G. Young, Sam T. Chao, Jean-Paul Daris, Gregory S. Bisacchi, Richard J. Colonno, C. Bachard, Philippe Lapointe, Z. Merchant |
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| Rok vydání: | 1997 |
| Předmět: |
Hepatitis B virus
biology Stereochemistry digestive oral and skin physiology Organic Chemistry Clinical Biochemistry Pharmaceutical Science biology.organism_classification medicine.disease_cause Biochemistry Chemical synthesis Thymine stomatognathic diseases chemistry.chemical_compound chemistry Hepadnaviridae Drug Discovery medicine Molecular Medicine Deoxyguanosine Enantiomer Enantiomeric excess Cytotoxicity Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 7:127-132 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(96)00594-x |
| Popis: | BMS-200475, a novel carbocyclic analog of 2′-deoxyguanosine, is a potent inhibitor of hepatitis B virus in vitro (ED50 = 3 nM) with relatively low cytotoxicity (CC50 = 21–120 μM). A practical 10-step asymmetric synthesis was developed affording BMS-200475 in 18% overall chemical yield and >99% optical purity. The enantiomer of BMS-200475 as well as the adenine, thymine, and iodouracil analogs are much less active. |
| Databáze: | OpenAIRE |
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