A series of 1-aryl-6, 7-dihydroxyl (methoxy)-1, 2, 3, 4-tetrahydroisoquinolines (compounds 1– 36) were synthesized via Pictet–Spengler cyclization. All the synthesized compounds were assayed for activities against HIV-1IIIB in C8166 cell cultures by MTT method for the first time. The results of the anti-HIV screening revealed that 6, 7- dihydroxytetrahydroisoquinolines possessed higher selective index than 6, 7-dimethoxyl ...