取代的四氢-β-咔啉类化合物作为治疗人乳头瘤病毒感染的潜在药物。

Substituted tetrahydro-beta-carbolines as potential agents for the treatment of human papillomavirus infection.

机构信息

Department of Medicinal Chemistry, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA.

出版信息

Bioorg Med Chem Lett. 2010 Jan 1;20(1):256-9. doi: 10.1016/j.bmcl.2009.10.123. Epub 2009 Oct 30.

DOI:10.1016/j.bmcl.2009.10.123

Abstract

The identification and optimization of a series of substituted tetrahydro-beta-carbolines with potent activity against human papillomavirus is described. Structure-activity studies focused on the substitution pattern and chirality of the beta-carboline ring system are discussed. Optimization of these parameters led to compounds with antiviral activities in the low nanomolar range.

摘要

描述了一系列具有抗人乳头瘤病毒活性的取代四氢-β-咔啉的鉴定和优化。讨论了β-咔啉环系统的取代模式和手性的构效关系研究。对这些参数的优化导致了具有纳摩尔级抗病毒活性的化合物。

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