BMS-200475, a novel carbocyclic 2′-deoxyguanosine analog with potent and selective anti-hepatitis B virus activity in vitro

…, O Kocy, P Lapointe, A Martel, Z Merchant…

文献索引：Bisacchi; Chao; Bachard; Daris; Innaimo; Jacobs; Kocy; Lapointe; Martel; Merchant; Slusarchyk; Sundeen; Young; Colonno; Zahler Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 2 p. 127 - 132

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被引用次数: 135

摘要

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.