Structure-activity relationships of nucleoside analogues for inhibition of tick-borne encephalitis virus
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- 作者：Luděk Eyera ; Marké ; ta &Scaron ; mí ; dková ; b ; Radim Nenckab ; Jiří ; Nečaa ; Tomá ; &scaron ; Kastla ; Martin Palusa ; d ; Erik De Clercqc ; Daniel Růžeka ; d ; ruzekd@paru.cas.cz" class="auth_mail" title="E-mail the corresponding author
- 关键词：Structure-activity relationship ; Tick-borne encephalitis ; Nucleoside inhibitor ; Antiviral activity ; Cytotoxicity
- 刊名：Antiviral Research
- 出版年：2016
- 出版时间：September 2016
- 年：2016
- 卷：133
- 期：Complete
- 页码：119-129
- 全文大小：2974 K
文摘
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A series of 29 nucleosides was evaluated for anti-TBEV/cytotoxicity effects using standardised in vitro assay systems.
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A relatively stringent structure-activity relationship exists for modifications at the 2′, 3′, and 4′ nucleoside positions.
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Some structure-activity relationship flexibility was found for changes of the purine/pyrimidine heterobase identity.
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Structural modifications of the heterobase were accompanied by either inefficacy against TBEV or cytotoxicity.
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C2′ methyl or C4′ azido substituents are crucial for a highly selective TBEV inhibition and a low cytotoxicity in vitro.