HIV encodes three enzymes: reverse transcriptase (RT), protease (PR), and integrase (IN). IN is a promising target because integration is an essential step in retroviral replication cycle. HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor. HIV-1 integrase inhibitor 8 inhibited 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. Furthermore, HIV-1 integrase inhibitor 8 inhibited MCV (molluscum contagiosum virus) topoisomerase and DNA religation with IC50 values of 500 µM and 200 µM, respectively. Moreover, HIV-1 integrase inhibitor 8 induced cell cytotoxicity and yielded a LD50 (dose at which the signal was reduced 50% due to cell death) of 20 μM in HeLa cells[2].
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