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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