Table 1.
Adenosine Deaminase Inhibitor | Ki Value (or IC50) |
Ref. |
---|---|---|
Transition-state inhibitors | ||
Coformycin | 10 pM | [50] |
2′-Deoxycoformycin | 2.5 pM | [51] |
4R-(1-Hydroxyethyl)-5-methyl-1-β-D-ribofuranosylimidazole | 61 µM | [52] |
2′-Chloro-2′deoxyadenosine (cladribine) | (0.2 µM) | [53,54] |
2′-Chloro-2′deoxycoformycin | 0.53 nM | [55] |
Adecypenol | 47 nM | [56] |
Ground-state inhibitors | ||
1-Deazaadenosine | 0.66 µM | [57] |
2′-Deoxy-1-deazaadenozine | 0.19 µM | [58] |
N6-Hydroxy-2′deoxy-1-deazaadenozine | 0.25 µM | [59] |
N6-Methyl-2′deoxy-1-deazaadenozine | 1.2 µM | [59] |
N6-Cyclopropyl-2′deoxy-1-deazaadenozine | 5.9 µM | [59] |
3′-Deoxy-1-deazaadenosine | 2.6 µM | [60] |
2′3′-Dideoxy-1-deazaadenosine | 2.2 µM | [60] |
Erythro-9-(2-hydroxy-3-nonyl) adenine (EHNA) | 1.6 nM | [61] |
9′-Chloro-EHNA | 2.7 nM | [62] |
9′-Phthalimido-EHNA | 0.95 nM | [62] |
Fluorescent derivatives of epsilon-EHNA | 2.8 µM | [63] |
1-DeazaEHNA | 0.16 µM | [64] |
3-DeazaEHNA | 0.01 µM | [64] |
Erythro-1-(2-hydroxy-3-nonyl)imidazole | 0.90 µM | [65] |
Erythro-9-(2-hydroxy-3-nonyl)imidazole-4-carboxamide | 0.035 µM | [65] |
Erythro-9-(2-hydroxy-3-nonyl)1,2,4-triazole | 0.3 µM | [66] |
Non-nucleoside inhibitors | ||
1-(1-Hydroxy-4-phenylbutan-2-yl)-1H-imidazole-4-carboxamide | 5.9 µM | [67] |
1-((1R,2S)-2-Hydroxy-1-(2-(1-naphthyl)ethyl)propyl)-1H-imidazole-4-carboxamide (FR234938) | 3.6 nM | [68] |
Flavonoids and sapogenins/plant extracts | ||
Kaempherol | (30 µM) | [69] |
Quercetin | (30 µM) | [69] |
Hibifolin | 50 µM | [70] |
Naringrin | 200 µM | [71] |
Curcumin | (13.6 µM) | [72] |
Genistein | (1.5 mM) | [73] |
Cyanidin-3-rutinoside | (0.95 mM) | [73] |
Acidic sapogenins 3-(4-Nitrophenyl)-5-phenyl isoxazole |
1 µM (0.380 mM) |
[74] [75] |
Drugs | ||
Acetaminophen | 214 µM | [76] |
Diclofenac | 30 µM | [77] |
Aspirin | 43 µM | [77] |
Lidoflazine | 30 µM | [78] |
Phenylbutazone | 54 µM | [78] |
Chlordiazepoxide | 83 µM | [78] |
Tradozon | 60 µM | [79] |