TABLE 1.

Anti-VV activities of various ANPs, in PHKs

CompoundCC50 (μg/ml)IC50 (μg/ml)SI
9-[2-(Phosphonomethoxy)ethyl]adenine (PMEA)12.3>50<0.2
PMEA di(isooctyl)ester12.991.4
9-[2-(Phosphonomethoxy)ethyl]-2,6-diaminopurine (PMEDAP)31.330.51.0
9-[2-(Phosphonomethoxy)ethyl]guanine (PMEG)0.11.1 ± 0.20.1
Isopropyl 9-[2-(phosphonomethoxy)ethyl]guanine13.6>50<0.3
9-[2-(Phosphonomethoxy)ethyl]-8-azaguanine6.4 ± 0.716.3 ± 11.00.4
1-[2-(Phosphonomethoxy)ethyl]-2,4-diaminopyrimidine17.78.0 ± 4.22.2
6-[2-(Phosphonomethoxy)ethoxy]-2,4-diaminopyrimidine21.714.0 ± 1.41.6
9-[2-(Phosphonomethoxy)ethyl]-2-amino-6-chloropurine hydrobromide0.92.7 ± 0.90.3
9-[2-(Phosphonomethoxy)ethyl]-2-amino-6-methylaminopurine8.937.0 ± 4.20.2
9-[2-(Phosphonomethoxy)ethyl]-2-amino-6-methylaminopurine5≥30.5 ± 27.6≤0.2
9-[2-(Phosphonomethoxy)ethyl]-2-amino-6-n-butylaminopurine11.32.44.7
9-[2-(Phosphonomethoxy)ethyl]-2-amino-6-allylamino purine0.97.3 ± 5.20.1
9-[(2-Phosphonomethoxy)ethyl]-2-amino-4-propargylaminopurine2.922.8 ± 20.20.1
9-[2-(Phosphonomethoxy)ethyl]-2-amino-6-cyclopropylaminopurine1.312.3 ± 5.30.1
9-[2-(Diisooctylphosphonylmethoxy)ethyl]-2-amino 6-cyclopropylaminopurine9.7101.0
9-[2-(Phosphonomethoxy)ethyl]-2-amino-6-cyclopentylaminopurine7.1≥45 ± 7≤0.2
9-[2-(Phosphonomethoxy)ethyl]-2-amino-6-dimethylaminopurine1.55.3 ± 3.30.3
9-[2-(Phosphonomethoxy)ethyl]-2-amino-6-(N-methyl, N-ethyl)aminopurine2.2 ± 0.210.7 ± 3.20.2
9-[2-(Phosphonomethoxy)ethyl]-2-amino-N6-(piperidin-1-yl)purine>41 ± 13>50 ± 0>0.8
9-(R)-[2-(Phosphonomethoxy)propyl]-6-dimethylaminopurine13.9>50 ± 0<0.3
9-(S)-[2-(Phosphonomethoxy)propyl]-2-amino-6-cyclopropylaminopurine15.9≥44.0 ± 10.4≤0.4
9-(S)-[2-(Phosphonomethoxy)propyl]guanine [(S)-PMPG]5.330 ± 00.2
1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]cytosine [(S)-HPMPC]≥34 ± 204.0 ± 2.6≥8.5
Cyclic -(S)-HPMPC≥41 ± 138.0 ± 6.0≥5.1
9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine [(S)-HPMPA]16.40.65 ± 0.3325.2
Cyclic (S)-HPMPA17.2 ± 1.31.3 ± 0.313.2
9-(S)-[(3-hydroxy-2-(phosphonomethoxy)propyl]-8-azaadenine8.37.5 ± 3.51.1
9-(S)-[(3-hydroxy-2-(phosphonomethoxy)propyl]-3-deazaadenine [3-deaza-(S)-HPMPA]7.3 ± 3.81.5 ± 1.14.9
Cyclic 3-deaza-(S)-HPMPA12.1 ± 3.81.7 ± 0.57.1
9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]guanine [(S)-HPMPG]7.5 ± 7.12.1 ± 1.93.6
Cyclic (S)-HPMPG8.23.8 ± 1.82.2
9-(R)-[3-hydroxy-2-(phosphonomethoxy)propyl]guanine [(R)-HPMPG]34.420 ± 01.7
Cyclic (R)-HPMPG13.616.5 ± 4.90.8
9-(RS)-[3-hydroxy-2-(phosphonomethoxy)propyl]guanine [(RS)-HPMPG]6.64.6 ± 2.71.4
9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-2,6-diaminopurine [(S)-HPMPDAP]>42.5 ± 10.82.7 ± 1.2≥16
9-(RS)-[3-hydroxy-2-(phosphonomethoxy)propyl]-6-hydroxylaminopurine [(RS)-HPMPDAP]17.33.5 ± 2.14.9
9-(RS)-[3-azido-2-(phosphonomethoxy)propyl]-2,6-diaminopurine>5011.5 ± 4.9>4.3