Table 3. Analogues with Modifications on Two Phenyl Rings.
compd | X | R1 | R2 | R3 | Inhibition of basal ATPase activity Kiapp (nM) | LE | K562 cells GI50 (nM) |
---|---|---|---|---|---|---|---|
8a | S | 3-OH | H | H | 200.3 ± 51.9 | 0.38 | 555 ± 121 |
43a | S | 3-CN | H | H | 542.4 ± 41.3 | 0.34 | 2128 ± 108 |
9a | S | 3-CONH2 | H | H | 419.7 ± 38.8 | 0.33 | 802 ± 51 |
44 | S | 4-Me | 4-Me | H | 56.0 ± 5.0 | 0.40 | 2174 ± 119 |
rac-45 | S | 3-OH | 3-Cl | H | 200.3 ± 35.3 | 0.37 | 1662 ± 77 |
rac-46 | S | 3-OH | 3-Et | H | 4.8 ± 1.2 | 0.44 | 260 ± 19 |
rac-47 | S | 3-OH | 4-Me | H | 7.1 ± 1.8 | 0.44 | 98 ± 6 |
rac-48 | S | 3-CN | 4-Me | H | 64.2 ± 5.2 | 0.38 | 1186 ± 34 |
rac-49 | S | 3-CONH2 | 4-Me | H | 55.6 ± 8.0 | 0.37 | 308 ± 16 |
dia-50 | C | 3-OH | 4-Me | CO2H | 7.8 ± 2.0 | 0.39 | 813 ± 20 |
rac-51 | C | 3-OH | 4-Me | H | 33.6 ± 6.4 | 0.41 | 232 ± 24 |
Values provided for reference from previous paper.29