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. 2020 Oct 12;25(20):4652. doi: 10.3390/molecules25204652

Table 1.

The main classes of adenosine deaminase inhibitors with inhibitory constant (Ki) value or the half maximal inhibitory concentration (IC50).

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]