Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication

被引:27
作者
Slater, MJ [1 ]
Baxter, R [1 ]
Bonser, RW [1 ]
Cockerill, S [1 ]
Gohil, K [1 ]
Parry, N [1 ]
Robinson, E [1 ]
Randall, R [1 ]
Yeates, C [1 ]
Snowden, W [1 ]
Walters, A [1 ]
机构
[1] GlaxoSmihKline, Med Res Ctr, Stevenage SG1 2NY, Herts, England
关键词
D O I
10.1016/S0960-894X(01)00352-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and antiviral evaluation of unsymmetrical indolocarbazole derivatives of Arcyriaflavin A, substituted with a range of alkyl groups at the indole nitrogen, is described. Structure-activity relationships in this series against human cytomegalovirus (HCMV) replication in cell culture are reported. Compound 4b was identified as potent inhibitor of HCMV (IC50 = 19 nM), which retained activity against a range of HCMV strains including ganciclovir resistant isolates. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1993 / 1995
页数:3
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