Table 1 Inhibition of integration strand transfer, anti-HIV activity and cytotoxicity in the HIV infected H9 cell line of the tested HIV-1 integrase inhibitors.
From: HIV-1 integrase inhibitors are substrates for the multidrug transporter MDR1-P-glycoprotein
Compound (DKA derivatives) | Strand Transfer IC50* (μM) | Anti-HIV activity EC50§ (μM) | Cytotoxicity CC50^ (μM) |
|---|---|---|---|
RDS 1974 | 32 | >50 | >50 |
RDS 1981 | 0.45 | >50 | >50 |
RDS 1983 | 0.25 | 5.98 | >50 |
RDS 1984 | 0.019 | 9.64 | >50 |
RDS 1992 | 0.70 | 20.5 | >50 |
RDS 1996 | 0.34 | 24.79 | 2.80 |
RDS 1997 | 0.012 | 2.44 | >50 |
RDS 2012 | 0.54 | 1.83 | >50 |
RDS 2022 | 0.042 | >50 | >50 |