714963-89-0Relevant articles and documents
α,α-Trehalose derivatives bearing guanidino groups as inhibitors to HIV-1 Tat-TAR RNA interaction in human cells
Wang, Min,Xu, Zhidong,Tu, Pengfei,Yu, Xiaolin,Xiao, Sulong,Yang, Ming
, p. 2585 - 2588 (2007/10/03)
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 6,6 ′-diamino-6,6′-dideoxy-α,α- trehalose was obtained from selective bromination of, α,α-trehalose at C-6,6′, 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 α,α-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.