HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8[1].
HIV-1 integrase inhibitor 8 is against 3′-processing (TC) and strand-transfer (ST) activities in the presence of Mn2+ as the cationic cofactor by gel assay with IC50 values of 275 µM and 200 µM, respectively. It inhibits the strand-transfer (ST) activity with an IC50 value of 200 µM[1].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 IC50 values of 500 µM and 200 µM, respectively. This result demonstrates that compound 8 is inactive against topoisomerase in both assays[1]. HIV-1 integrase inhibitor 8 induces cell cytotoxicity and yields a LD50 (dose at which the signal is reduced 50% due to cell death) of 20 μM in HeLa cells[1].
[1]. Molteni, et al. A New Class of HIV-1 Integrase Inhibitors: The 3,3,3’, 3’-tetramethyl-1,1’-spirobi(indan)-5,5’,6,6’-tetrol Family.J Med Chem