A　series　of　aromatic　diketone　derivatives　were　designed　and　synthesized　as　potential　HIV-1　integrase　(IN)　inhibitors　and　evaluated　to　determine　their　ability　to　inhibit　the　strand　transfer　process　of　HIV-1　integrase.　The　results　indicate　that　(Z)-1-(3-acetyl-2-hydroxy-4,6-dimethoxyphenyl)-3-hydroxy-3-(substituted)　phenylprop-2-en-1-one　(5a-5d)　can　moderately　inhibit　HIV-1　integrase.　The　cyclization　and　condensation　products　(6a-6c　and　7e-7f)　of　compounds　5a-5d　show　poor　inhibitory　activity　against　HIV-1　integrase.　The　molecular　docking　results　indicate　that　the　different　types　of　compounds　act　on　HIV-1　integrase　in　different　ways,　and　these　results　can　explain　the　differences　in　the　inhibitory　activities.