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一种新型碳环核苷类似物(卡波韦:NSC 614846)在体外对人类免疫缺陷病毒具有强效和选择性活性。

Potent and selective activity of a new carbocyclic nucleoside analog (carbovir: NSC 614846) against human immunodeficiency virus in vitro.

作者信息

Vince R, Hua M, Brownell J, Daluge S, Lee F C, Shannon W M, Lavelle G C, Qualls J, Weislow O S, Kiser R

机构信息

Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis 55455.

出版信息

Biochem Biophys Res Commun. 1988 Oct 31;156(2):1046-53. doi: 10.1016/s0006-291x(88)80950-1.

Abstract

Carbocyclic 2',3'-didehydro-2',3'-dideoxyguanosine (Carbovir: NSC 614846), a novel nucleoside analog, emerged as a potent and selective anti-HIV agent from a large screening program conducted by the National Cancer Institute and its contractors. Its hydrolytic stability and its ability to inhibit the infectivity and replication of HIV in T-cells at concentrations of approximately 200- to 400-fold below toxic concentrations make carbovir a top-priority candidate for development as a potential antiretroviral agent in the treatment of AIDS patients.

摘要

碳环2',3'-二脱氢-2',3'-二脱氧鸟苷(卡波韦:NSC 614846)是一种新型核苷类似物,它是美国国立癌症研究所及其承包商开展的一项大型筛选计划中发现的一种强效且具有选择性的抗HIV药物。其水解稳定性以及在毒性浓度约低200至400倍的浓度下抑制HIV在T细胞中的感染性和复制的能力,使卡波韦成为开发用于治疗艾滋病患者的潜在抗逆转录病毒药物的首要候选药物。

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