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

被引：129

作者：

Bisacchi, GS

Chao, ST

Bachard, C

Daris, JP

Innaimo, S

Jacobs, GA

Kocy, O

Lapointe, P

Martel, A

Merchant, Z

Slusarchyk, WA

Sundeen, JE

Young, MG

Colonno, R

Zahler, R

机构：

[1] Bristol-Myers Squibb P., Princeton, NJ 08543-4000

[2] Bristol-Myers Squibb P., Candiac, Que. J5R 1J1

[3] Bristol-Myers Squibb P., Wallingford, CT 06492-7660

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(96)00594-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 (CC50=21-120 mu M). A practical 10-step asymmetric synthesis was developed affording BMS-200475 in 18% overall chemical yield and >99% optical purity. The enantiomer of EMS-200475 as well as the adenine, thymine, and iodouracil analogs are much less active. (C) 1997, Elsevier Science Ltd.

引用

页码：127 / 132

页数：6

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