3,3,3',3'-四甲基-1,1'-螺BI(茚满)-6,6'-二醇

HIV-1 integrase inhibitor 8 is against 3′-processing (TC) and strand-transfer (ST) activities in the presence of Mn ²⁺ as the cationic cofactor by gel assay with IC ₅₀ values of 275 µM and 200 µM, respectively. It inhibits the strand-transfer (ST) activity with an IC ₅₀ value of 200 µM.The DNA relaxation activity of MCV topoisomerase is monitored by gel electrophoresis, while DNA cleavage and religation activities were monitored using a microtiter assay. HIV-1 integrase inhibitor 8 inhibits MCV topoisomerase and DNA religation with IC ₅₀ values of 500 µM and 200 µM, respectively. This result demonstrates that compound 8 is inactive against topoisomerase in both assays. HIV-1 integrase inhibitor 8 induces cell cytotoxicity and yields a LD ₅₀ (dose at which the signal is reduced 50% due to cell death) of 20 μM in HeLa cells.