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

G.S Bisacchi,S.T Chao,C Bachard,J.P Daris,S Innaimo,G.A Jacobs,O Kocy,P Lapointe,A Martel,Z Merchant,W.A Slusarchyk,J.E Sundeen,M.G Young,R Colonno,R Zahler

doi:10.1016/s0960-894x(96)00594-x

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

G.S Bisacchi, S.T Chao + Show 13 more

https://doi.org/10.1016/s0960-894x(96)00594-x

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Journal: Bioorganic & Medicinal Chemistry Letters	Publication Date: Jan 1, 1997
Citations: 150

Affiliation: Bristol-Myers Squibb (Canada), Bristol-Myers Squibb (United States)

#Potent Inhibitor Of Hepatitis #Deoxyguanosine Analog + Show 8 more

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Abstract

BMS-200475, a novel carbocyclic analog of 2′-deoxyguanosine, is a potent inhibitor of hepatitis B virus in vitro (ED 50 = 3 nM) with relatively low cytotoxicity (CC 50 = 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.

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