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. Author manuscript; available in PMC: 2008 Sep 11.
Published in final edited form as: J Med Chem. 2007 Mar 21;50(8):1828–1839. doi: 10.1021/jm061304k

Table 3.

In vitro anti-HIV-1 activity and toxicity of d-3′,3′-difluoro-2′,3′-dideoxy-carbocyclic nucleosides and d- & l- 3′-fluoro-2′,3′-didehydro-carbocyclic nucleosides.

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B Configuration Anti-HIV-1 activity (μM)a Cytotoxicity (μM)
EC50 EC90 PBM CEM Vero
Adenine 31 D >100 >100 95.1 >100 >100
Guanosine 32 D >100 >100 >100 >100 >100
Hypoxanthine 33 D >100 >100 >100 >100 >100
Cytosine 37 D >100 >100 >100 >100 >100
Thymine 38 D >100 >100 >100 >100 >100
Cytosine 18 L 7.1 72.0 >100 >100 >100
Thymine 19 L 6.4 >100 >100 >100 >100
Adenine 26 L 10.3 33.5 >100 >100 >100
Hypoxanthine 27 L >100 >100 >100 >100 >100
Guanine 28 L 20.7 >100 >100 >100 >100
Adenine 34 D 14.8 40.6 >100 >100 >100
Guanine 35 D 0.41 2.8 21.1 >100 >100
Hypoxanthine 36 D >100 >100 >100 >100 >100
Cytosine 39 D >100 >100 >100 >100 >100
Thymine 40 D 68.8 >100 >100 >100 >100
Carbovir D 0.087b 0.27b N/A N/A N/A
a

Anti-HIV activity evaluated in PBM cells against HIV-1LAI unless otherwise indicated.

b

Anti-HIV activity evaluated in PBM cells against HIV-1xxBRU.