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. Author manuscript; available in PMC: 2018 Jan 22.
Published in final edited form as: J Med Chem. 2016 Jul 22;59(15):7097–7110. doi: 10.1021/acs.jmedchem.6b00428

Table 3.

HIV-1 Activity of Lipid Conjugates 14–22 in PBMCsa

compd R– EC50b (PBMCs) CC50c (PBMCs) TI (CC50/EC50)
TDF NA 0.0046 43.7 9500
TFV NA 0.319 >100.0 >300
14 MeO– 0.026 38.2 1500
15 EtO– 0.349 36.2   104
16 PrO– 0.216 10.6     49.0
17 n-BuO– 0.19 27.9   150
18 s-BuO– 0.049 23.7   480
19 C(CH3)3CH2O– 0.14 >100.0 >700
20 PhCH2O– 0.018 41.1 2300
21 PhNH– 0.005 34.2 7000
22 C8H17O– 0.911 >50.0   >50
a

All data represent an average of triplicate experiments.

b

EC50, effective concentration (in μM) required to inhibit HIV-1 by 50%.

c

CC50, effective concentration (in μM) required to reduce the viability of uninfected cells by 50%.