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. Author manuscript; available in PMC: 2013 Dec 17.
Published in final edited form as: Bioorg Med Chem. 2011 Mar 1;19(6):10.1016/j.bmc.2011.01.047. doi: 10.1016/j.bmc.2011.01.047

Table 3.

Anti-HIV activity of selected novel potent derivatives

Comp. in Anti-HIV-1 activity in PBMCsa Slope R Cytotoxicity (IC50, μM)
EC50 (μM)b EC90 (μM)b PBMCs CEM
15 8.7 21.0 2.5±0.61 0.97 24.4 27.5
17 13.9 26.0 3.5 1.0 22.1 23.8
25 7.3 20.3 2.2±0.96 0.91 22.7 19.0
49 10.1 24.3 2.5±0.89 0.94 39.1 20.7
8 30.8 52.7 4.1 1.0 44.0 40.2
AZT 0.0025 0.01 1.6±0.30 0.96 >100 56.1
L-706,908 5.7±4.7c N/A N/A N/A N/A N/A
a

Human peripheral blood mononuclear cells(PBMCs),

b

EC50 and EC90 are the effective concentrations inhibiting 50% and 90% HIV replication, respectively.

c

In the human leukemic T–cell line MOLT -4; in that assay the EC50 of AZT was 0.001 μM.