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.
He
Meizi
M
National Research Laboratory of Natural and Biomimertic Drugs, Peking University, Beijing 100083, China.
Yuan
Dekai
D
Lin
Wei
W
Pang
Ruifang
R
Yu
Xiaolin
X
Yang
Ming
M
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D019075:Electrophoresis, Capillary; D015696:Gene Products, tat / Q000187:drug effects* / Q000378:metabolism; D016325:HIV Long Terminal Repeat / Q000187:drug effects*; D006801:Humans; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D011485:Protein Binding / Q000187:drug effects; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D015696:Gene Products, tat; D007546:Isoquinolines