Table 1.
Ki Values of Compounds 10–31 and Archival Compounds 9, 75, and 76 in the Inhibition of Soluble hCD73 or as Otherwise Noted (triethylammonium salts were prepared and tested)c
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No. | Structure R1 = (other changes) |
Ki ± SEM (nM, n=3) |
9 |
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10.6 ± 0.4a, 3.67 ± 0.26a,b |
10 |
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1.63 ± 0.28 |
11 |
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1.58 ± 0.06 |
12 |
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1.27 ± 0.18 |
13 |
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0.894 ± 0.175 |
14 |
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3.50 ± 0.11 |
15 |
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1.14 ± 0.06 |
16 |
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0.673 ± 0.091 |
17 |
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0.441 ± 0.157 |
18 |
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0.436 ± 0.078 |
19 |
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1.08 ± 0.34 |
20 |
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0.511 ± 0.041 |
21 |
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0.848 ± 0.229 |
22 |
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14.1 ± 2.9 |
23 |
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1.76 ± 0.43 |
24 |
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0.626 ± 0.076 |
25 |
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1.78 ± 0.33 |
26 |
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2.51 ± 0.51 |
27 |
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2.61 ± 0.94 (n=2) |
28 | O | > 50 μM (28% inhibition) |
29 |
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59.2 ± 5.58 |
30 |
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71.5 ± 17.6 |
31 | O, R2 = F | 2540 ± 710 |
75 | O, R2 = CH3 | 338 ± 56a,b |
76 |
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4.58 ± 0.55a, 13.9 ± 1.6a,b |