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. Author manuscript; available in PMC: 2018 Jan 22.
Published in final edited form as: J Med Chem. 2016 Nov 2;59(22):10244–10252. doi: 10.1021/acs.jmedchem.6b01292

Table 1.

HIV-1 and HBV Activity of Conjugates 1–5b, 6, and 7 Compared to TFV and TDFa

HIV-l
HBV
Ident. Structure EC50b (PBMCs) CC50b(PBMCs) TI (CC50/EC50) EC50b (HepG2) CC50b (HepG2) TI (CC50/EC50)
TFV graphic file with name nihms932320t1.jpg 0.320 > 100 >300 – – –
TDF graphic file with name nihms932320t2.jpg 0.0045 44.0 9500 0.34 64.5 190
1b graphic file with name nihms932320t3.jpg 0.00065 14.3 22000 0.020 >25 > 1200
2b graphic file with name nihms932320t4.jpg < 0.0005 >50 >100000 0.248 >50 >200
3b graphic file with name nihms932320t5.jpg 0.0229 17.2 751 4.48 17.5 3.9
4b graphic file with name nihms932320t6.jpg < 0.0005 15.9 >31800 0.152 32.5 214
5b graphic file with name nihms932320t7.jpg 0.007 >50 >7000 1.05 >50 >47
6 graphic file with name nihms932320t8.jpg 18.6 > 100 >5.38 41.9 >100 >2
7 graphic file with name nihms932320t9.jpg 5.13 > 100 > 18 > 100 > 100 > 1
a

All data represent an average of triplicate experiments. R = tenofovir.

b

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

c

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