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. 2013 Feb 11;56(5):1878–1893. doi: 10.1021/jm3014597

Table 3. Analogues with Modifications on Two Phenyl Rings.

graphic file with name jm-2012-014597_0003.jpg

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
a

Values provided for reference from previous paper.29