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. Author manuscript; available in PMC: 2011 Dec 15.
Published in final edited form as: Bioconjug Chem. 2010 Nov 15;21(12):2239–2249. doi: 10.1021/bc1002168

Table 1.

Effects of various nucleosides and their conjugates 10a-h against HIV-1 and their cytotoxicity assays.

Analog Nucleoside/Conjugate (source) Anti-HIV-1 activity in PBM cellsa
Cytotoxicity (IC50 [μM])b
EC50 [μM] EC90 [μM] PBM cells CEM cells VERO cells
AZT (commercial) 0.0054 0.050 > 100 14.3 56.0
d4U (synthesized) > 100 > 100 > 100 55.9 > 100
10a Glc-d4U > 100 > 100 > 100 > 100 > 100
d4T (commercial) 0.073 0.37
d4T (synthesized) 0.069 0.37 > 100 > 100 > 100
10b Glc-d4T 0.34 2.0 > 100 76.8 > 100
IdUrd (commercial) 65.7 > 100
IdUrd (synthesized) 86.5 > 100 > 100 2.7 > 100
10c Glc-5′-IdUrd 32.4 > 100 > 100 2.3 > 100
10d Glc-3′-IdUrd > 100 > 100 > 100 76.0 > 100
ddI (commercial) 0.32 2.8
ddI (synthesized) 0.06 0.76 > 100 > 100 > 100
10e Glc-ddI 15.5 > 100 > 100 22.7 > 100
ddA (synthesized) 0.59 3.8 > 100 > 100 > 100
10f Glc-ddA 1.1 9.9 87.6 13.2 73.2
Virazole (commercial) 77.5 > 100
Virazole (synthesized) 85.9 > 100 > 100 53.0 > 100
10g Glc-Virazole 12.8 39.1 > 100 17.6 > 100
Ara-A (commercial) > 100 > 100
Ara-A (synthesized) > 100 > 100 26.0 26.2 > 100
10h Glc-Ara-A 19.5 > 100 > 100 18.9 > 100
Ara-C (synthesized) 4.9 11.9 57.0 < 0.1 ND
10i Glc-Ara-C 5.8 14.0 17.5 < 1.0 < 1.0
a

HIV drug susceptibility assay was done as previously described in reference (45).

b

Cytotoxicity assays in PBM, CEM and Vero cells were done as previously described in reference (46). ND = not determined