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

Table 2. Analogues Containing Disubstituted Phenyl Rings.

graphic file with name jm-2012-014597_0002.jpg

compd X R1 R2 R3 inhibition of basal ATPase activity Kiapp (nM) LE K562 cells GI50 (nM)
28 S 2-F 3-Me H 293.6 ± 23.2 0.36 2547 ± 141
29 S 2-F 4-Me H 201.3 ± 18.7 0.37 2084 ± 109
30 S 2-F 4-OMe (R)-CO2H 10.4 ± 4.5 0.38 82 ± 3
31 S 2-F 4-OMe H 11.6 ± 3.7 0.42 489 ± 26
32 S 3-F 4-OMe H 162.2 ± 15.6 0.36 1892 ± 134
33 S 3-Cl 4-Cl H 35.2 ± 4.9 0.41 1993 ± 343
34 S 3-Me 4-Me (R)-CO2H 1.2 ± 0.1 0.43 72 ± 8
35 S 3-Me 4-Me H 25.7 ± 6.3 0.41 729 ± 43
36 S 3-Et 4-Me (R)-CO2H 4.6 ± 1.7 0.39 34 ± 2
37 S 3-Et 4-Me H 7.8 ± 3.9 0.43 1045 ± 42
38 S 3,4-(CH2)4 (R)-CO2H 2.1 ± 0.5 0.40 56 ± 2
39 S 3,4-(CH2)4 H 10.6 ± 3.2 0.40 934 ± 127
40 C 2-F 4-OMe H 37.9 ± 4.7 0.39 764 ± 42
41 C 3-Cl 4-Cl H 31.4 ± 6.4 0.41 633 ± 126
rac-42 C 3-Me 4-Me CO2H 12.4 ± 4.4 0.38 23.4 ± 1.8