a, a-Trehalose derivatives bearing guanidino groups as inhibitors to HIV-1 Tat-TAR RNA interaction in human cells，成果详细信息-中国科技论文在线

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a, a-Trehalose derivatives bearing guanidino groups as inhibitors to HIV-1 Tat-TAR RNA interaction in human cells

杨铭， Min Wang ， a ， b Zhidong Xu ， b Pengfei Tu ， a Xiaolin Yu ， a Sulong Xiao a and Ming Yang a ， *

Bioorganic & Medicinal Chemistry Letters 14 (2004) 2585-2588，-0001，（）：

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摘要/描述

Replication of HIV-1 requires specific interactions of Tat protein with TAR RNA. Disruption of Tat-TAR RNA interaction could inhibit HIV-1 replication. Here four target compounds were designed and synthesized to bind to TAR RNA for blocking the interaction of Tat-TAR RNA. The core molecule 6,60-diamino-6,60-dideoxy-a,a-trehalose was obtained from selective bromination of, a,a-trehalose at C-6,60, followed by acetylation, azide displacement, deacetylation, and reduction. Coupling of the core molecule with the protected amino acid, then deprotection and guanidinylation generated the novel a,a-trehalose derivatives. Their abilities to inhibit Tat-TAR RNA interaction in human cells were determined by a Tat-dependent HIV-1 LTR-driven CAT assays.

关键词: a,a-Trehalose; Guanidino groups; Tat-TAR interaction; *Corresponding author ，

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