Synthesis and assay of isoquinoline derivatives as HIV-1 Tat–TAR interaction inhibitors

Four new isoquinoline derivatives bearing guanidinium group or amino group-terminated side chain were synthesized to target the HIV-1 TAR element. Their abilities to bind TAR RNA and inhibit Tat–TAR RNA interaction were determined by CE analysis, a Tat-dependent HIV-1 LTR-driven CAT assay and SIV-induced syncytium evaluation.

Graphical abstractSynthesis and biological evaluation of a series of isoquinoline derivatives are described. The compound IG2 bearing guanidinium group-terminated side chain can block the HIV-1 Tat–TAR RNA interaction and exhibit the antiviral potency.Figure optionsDownload full-size imageDownload as PowerPoint slide