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Table 2 Fhit inhibition by AppppA analogs varied in phosphorothiolation and three modifications of glycerol.

From: Di-, tri- and tetra-5'-O-phosphorothioadenosyl substituted polyols as inhibitors of Fhit: Importance of the α-β bridging oxygen and β phosphorus replacement

    
     X = O X = S
Comp R1 R2 R3 Ki (nm) Ki (nM)
     a b
6 O OH H 4700 35
7 O CH3 H - 76000
8 O NH3 H - 3000
9 O H H - 230
10 NH H H - 3300
11 S H H - 5200
12 O -CH2-O-P-(X,O)-OAdo -CH2-O-P-(X,O2) 1500 40
13 O -CH2-O-P-(X,O)-OAdo -CH2-O-P-(X,O)-OAdo 3200 65
14 O -CH2O-P-(X,O2) -CH2-O-P-(X,O2) 900 700
15 O -O-P-(X,O)-OAdo H 1500 78
16 NH -O-P-(X,O)-OAdo H - 2700
17 O -O-P-(X,O2) H 420 110