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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
  1. * 50% Inhibitory Concentration; § 50% Effective Concentration; ^ 50% Cytotoxic Concentration