Table 1.
Skeleton I | ||||||||
---|---|---|---|---|---|---|---|---|
Compound | R | R1 | R2 | R3 | R4 | R5 | X | Activity, (IC50µ M) |
1 | H | Me | H | - | - | - | - | 8.1 |
2 | H | H | Me | - | - | - | - | 0.10 |
3 | H | Cl | H | - | - | - | - | 0.55 |
4 | H | H | Cl | - | - | - | - | 0.0099 |
5 | H | NO2 | H | - | - | - | - | 3.0 |
6 | H | H | NO2 | - | - | - | - | 0.028 |
7 | H | H | O-Me | - | - | - | - | 0.35 |
8 | H | NH2 | H | - | - | - | - | 3.8 |
9 | H | H | F | - | - | - | - | 0.087 |
10 | H | Cl | Cl | - | - | - | - | 0.47 |
11 | H | O-Me | O-Me | - | - | - | - | 5.2 |
12 | CH2-Ph | Me | H | - | - | - | - | 3.7 |
13 | CH2-Ph | H | Me | - | - | - | - | 0.75 |
14 | CH2-Ph | H | Cl | - | - | - | - | 0.17 |
15 | CH2-Ph | NO2 | H | - | - | - | - | 1.6 |
16 | CH2-Ph | H | NO2 | - | - | - | - | 4.8 |
17 | C7H15 | Me | H | - | - | - | - | 0.39 |
18 | C7H15 | H | Me | - | - | - | - | 0.13 |
19 | C7H15 | H | Cl | - | - | - | - | 0.013 |
20 | C7H15 | H | NO2 | - | - | - | - | 0.29 |
21 | C7H15 | H | O-Me | - | - | - | - | 0.46 |
22 | C7H15 | H | F | - | - | - | - | 0.045 |
23 | H | H | H | - | - | - | - | 0.25 |
Skeleton II | ||||||||
Compound | R | R1 | R2 | R3 | R4 | R5 | X | Activity, (IC50μ M) |
24 | H | H | H | H | H | H | - | 0.68 |
25 | H | NO2 | H | H | H | H | - | >100 |
26 | H | NO2 | H | H | H | H | - | 5.9 |
27 | H | H | NO2 | H | H | H | - | 67.5 |
28 | H | H | NH2 | H | H | H | - | 29 |
29 | H | H | Cl | H | H | H | - | 6.5 |
30 | H | H | F | H | H | H | - | 1.2 |
31 | H | H | H | O-Me | H | H | - | 1.6 |
32 | H | H | H | H | O-Me | H | - | 6.5 |
33 | H | H | H | H | H | O-Me | - | 4.3 |
34 | H | H | H | Me | H | H | - | 3.9 |
35 | H | H | H | H | H | Me | - | 4.6 |
36 | H | H | H | H | F | H | - | 0.43 |
37 | H | H | H | H | Cl | H | - | 5.4 |
38 | CH2-Ph | H | H | H | H | H | - | 7.1 |
39 | Me | H | H | H | H | H | - | 1.3 |
40 | C7H15 | H | H | H | H | H | - | 4.3 |
Skeleton III | ||||||||
Compound | R | R1 | R2 | R3 | R4 | R5 | X | Activity, (IC50µ M) |
41 | - | - | - | - | - | - | CH2-CH2 | 2.98 |
42 | - | - | - | - | - | - | OCH2 | 245 |
43 | - | - | - | - | - | - | SCH2 | 18.58 |
44 | - | - | - | - | - | - | - | 11.48 |