Code numbersa,b | R or R1 | X | IC50 (MCF7, nM) | Competition assayc |
9 | R = 2-Me | O | 30 | ++ |
10 | R = 3-Me | O | 57 | +++ |
11 | R = 4-Me | O | 150 | − |
12 | R = 4-OMe | O | 160 | + |
13 | R = 4-NMe2 | O | 500 | N/A |
14 | R = 4-OH | O | >1000 | N/A |
15 | R = H | O | >1000 | N/A |
17 | R = 2-Prop | O | 69 | + |
18 | R = 2-OMe | O | 220 | N/A |
19 | R = 2-OEt | O | 83 | +++ |
21 | R = 2-F | O | 61 | ++ |
24 | R = 2-Me, 3-Me | O | 50 | +++ |
25 | R = 2-Me, 4-Me | O | 50 | + |
26 | R = 2-Me, 5-Me | O | 14 | +++ |
27 | R = 2-Me, 4-Me, 5-Me | O | 66 | ++ |
28 | R = 2-Cl, 4-Cl, 5-Cl | O | 30 | +++ |
29 | R = 2-Cl, 4-Cl, 6-Cl | O | 170 | N/A |
30 | R = 2-F, 4-F | O | 55 | ++ |
31 | R = 2-F, 6-F | O | 32 | +++ |
32 | R = 2-F, 3-F, 4-F, 5-F, 6-F | O | 320 | N/A |
34 | R = 3-OMe | O | 34 | +++ |
37 | R = 3-F | O | 54 | ++ |
38 | R = 3-I | O | 18 | +++ |
39 | R = 3-NO2 | O | 60 | +++ |
40 | R = 3-NH2 | O | 270 | N/A |
41 | R = 3-Me, 5-Me | O | 47 | +++ |
42 | R = 3-Me, 4-Me, 5-Me | O | 49 | +++ |
43 | R = 3-OMe, 4-OMe | O | 88 | +++ |
44 | R = 3-OMe, 5-OMe | O | 10 | +++ |
45 | R = 3-OMe, 4-OMe, 5-OMe | O | 5.0 | +++ |
46 | R = 3-Cl, 5-Cl | O | 18 | +++ |
47 | R = 3-F, 4-F | O | 100 | + |