Table 1. Structures and actual pIC50 (CDK4) and log[IC50 (CDK2)/IC50 (CDK4)] values of thieno[2,3-d]pyrim-idin-4-yl hydrazone analogues.
Compound | R1 | R2 | R3 | R4 | Actual |
|
---|---|---|---|---|---|---|
pIC50 (CDK4) | log[IC50 (CDK2)/IC50 (CDK4)] | |||||
1 | Et | H | H | 5.584 | 0.166 | |
2 | Me | H | H | 5.159 | −0.048 | |
3 | i-Pr | H | H | 6.781 | 0.845 | |
4 | t-Bu | H | H | 6.421 | 0.669 | |
5 | Me | Et | H | 4.276 | −0.125 | |
6 | i-Pr | H | Me | 5.053 | 0.502 | |
7 | Et | H | H | t-Bu | 4.775 | −0.064 |
8 | Et | H | H | 4.886 | 0.108 | |
9 | i-Pr | H | H | 5.528 | 0.547 | |
10 | i-Pr | H | H | 5.732 | 0.105 | |
11 | i-Pr | H | H | 6.093 | 0.138 | |
12 | i-Pr | H | H | Phenyl | 5.799 | 0.272 |
13 | i-Pr | H | H | 5.871 | 0.149 | |
14 | t-Bu | H | H | 5.539 | 0.493 | |
15 | t-Bu | H | H | 5.794 | 0.0492 | |
16 | t-Bu | H | H | 5.567 | 1.135 | |
17 | t-Bu | H | H | 5.796 | 1.123 | |
18 | t-Bu | H | H | 5.762 | 0.785 | |
19 | t-Bu | H | H | 6.152 | 1.453 | |
20 | t-Bu | H | H | 6.818 | 1.398 | |
21 | t-Bu | H | H | 6.382 | 1.51 | |
22 | t-Bu | H | H | 5.989 | 0.778 | |
23 | t-Bu | H | H | 5.558 | −0.4 | |
24 | t-Bu | H | H | 5.929 | −0.187 | |
25 | t-Bu | H | H | 7.15 | 1.626 | |
26 | t-Bu | H | H | 6.678 | 0.892 | |
27 | t-Bu | H | H | 7.152 | 1.015 | |
28 | t-Bu | H | H | 7.209 | 1.882 | |
29 | t-Bu | H | H | 6.969 | 1.253 | |
30 | t-Bu | H | H | 6.627 | 0.797 | |
31 | t-Bu | H | H | 6.58 | 1.018 | |
32 | t-Bu | H | H | 6.691 | 1.574 | |
33 | t-Bu | H | H | 7.032 | 0.724 | |
34 | t-Bu | H | H | 6.984 | 1.226 | |
35 | t-Bu | H | H | 6.888 | 0.688 | |
36 | t-Bu | H | H | 5.552 | 0.398 | |
37 | t-Bu | H | H | 6.785 | 0.041 | |
38 | t-Bu | H | H | 7.026 | 1.46 | |
39 | t-Bu | H | H | 6.934 | 0.919 | |
40 | t-Bu | H | H | 6.939 | 1.513 | |
41 | t-Bu | H | H | 6.586 | 0.623 | |
42 | t-Bu | H | H | 7.279 | 1.64 | |
43 | t-Bu | H | H | 6.812 | 1.382 | |
44 | t-Bu | H | H | 7.006 | 1.473 | |
45 | t-Bu | H | H | 6.708 | 1.137 | |
46 | t-Bu | H | H | 6.743 | 1.41 | |
47 | t-Bu | H | H | 7.457 | 2.084 | |
48 | t-Bu | H | H | 7.157 | 0.903 | |
49 | i-Pr | H | H | 6.777 | 1.413 | |
50 | H | H | 6.902 | 1.493 | ||
51 | H | H | 7.095 | 1.182 | ||
52 | H | H | 7.097 | 1.67 | ||
53 | H | H | 7.287 | 1.607 | ||
54 | H | H | 7.232 | 1.602 | ||
55 | H | H | 6.737 | 1.417 | ||
56 | H | H | 6.421 | 1.111 | ||
57 | H | H | e4r | 6.904 | 1.167 |