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. 2013 Oct 14;35(1):151–160. doi: 10.1038/aps.2013.105

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.Inline graphic

Compound R1 R2 R3 R4 Actual
pIC50 (CDK4) log[IC50 (CDK2)/IC50 (CDK4)]
1 Et H H graphic file with name aps2013105i2.jpg 5.584 0.166
2 Me H H graphic file with name aps2013105i3.jpg 5.159 −0.048
3 i-Pr H H graphic file with name aps2013105i4.jpg 6.781 0.845
4 t-Bu H H graphic file with name aps2013105i5.jpg 6.421 0.669
5 Me Et H graphic file with name aps2013105i6.jpg 4.276 −0.125
6 i-Pr H Me graphic file with name aps2013105i7.jpg 5.053 0.502
7 Et H H t-Bu 4.775 −0.064
8 Et H H graphic file with name aps2013105i8.jpg 4.886 0.108
9 i-Pr H H graphic file with name aps2013105i9.jpg 5.528 0.547
10 i-Pr H H graphic file with name aps2013105i10.jpg 5.732 0.105
11 i-Pr H H graphic file with name aps2013105i11.jpg 6.093 0.138
12 i-Pr H H Phenyl 5.799 0.272
13 i-Pr H H graphic file with name aps2013105i12.jpg 5.871 0.149
14 t-Bu H H graphic file with name aps2013105i13.jpg 5.539 0.493
15 t-Bu H H graphic file with name aps2013105i14.jpg 5.794 0.0492
16 t-Bu H H graphic file with name aps2013105i15.jpg 5.567 1.135
17 t-Bu H H graphic file with name aps2013105i16.jpg 5.796 1.123
18 t-Bu H H graphic file with name aps2013105i17.jpg 5.762 0.785
19 t-Bu H H graphic file with name aps2013105i18.jpg 6.152 1.453
20 t-Bu H H graphic file with name aps2013105i19.jpg 6.818 1.398
21 t-Bu H H graphic file with name aps2013105i20.jpg 6.382 1.51
22 t-Bu H H graphic file with name aps2013105i21.jpg 5.989 0.778
23 t-Bu H H graphic file with name aps2013105i22.jpg 5.558 −0.4
24 t-Bu H H graphic file with name aps2013105i23.jpg 5.929 −0.187
25 t-Bu H H graphic file with name aps2013105i24.jpg 7.15 1.626
26 t-Bu H H graphic file with name aps2013105i25.jpg 6.678 0.892
27 t-Bu H H graphic file with name aps2013105i26.jpg 7.152 1.015
28 t-Bu H H graphic file with name aps2013105i27.jpg 7.209 1.882
29 t-Bu H H graphic file with name aps2013105i28.jpg 6.969 1.253
30 t-Bu H H graphic file with name aps2013105i29.jpg 6.627 0.797
31 t-Bu H H graphic file with name aps2013105i30.jpg 6.58 1.018
32 t-Bu H H graphic file with name aps2013105i31.jpg 6.691 1.574
33 t-Bu H H graphic file with name aps2013105i32.jpg 7.032 0.724
34 t-Bu H H graphic file with name aps2013105i33.jpg 6.984 1.226
35 t-Bu H H graphic file with name aps2013105i34.jpg 6.888 0.688
36 t-Bu H H graphic file with name aps2013105i35.jpg 5.552 0.398
37 t-Bu H H graphic file with name aps2013105i36.jpg 6.785 0.041
38 t-Bu H H graphic file with name aps2013105i37.jpg 7.026 1.46
39 t-Bu H H graphic file with name aps2013105i38.jpg 6.934 0.919
40 t-Bu H H graphic file with name aps2013105i39.jpg 6.939 1.513
41 t-Bu H H graphic file with name aps2013105i40.jpg 6.586 0.623
42 t-Bu H H graphic file with name aps2013105i41.jpg 7.279 1.64
43 t-Bu H H graphic file with name aps2013105i42.jpg 6.812 1.382
44 t-Bu H H graphic file with name aps2013105i43.jpg 7.006 1.473
45 t-Bu H H graphic file with name aps2013105i44.jpg 6.708 1.137
46 t-Bu H H graphic file with name aps2013105i45.jpg 6.743 1.41
47 t-Bu H H graphic file with name aps2013105i46.jpg 7.457 2.084
48 t-Bu H H graphic file with name aps2013105i47.jpg 7.157 0.903
49 i-Pr H H graphic file with name aps2013105i48.jpg 6.777 1.413
50 graphic file with name aps2013105i49.jpg H H graphic file with name aps2013105i50.jpg 6.902 1.493
51 graphic file with name aps2013105i51.jpg H H graphic file with name aps2013105i52.jpg 7.095 1.182
52 graphic file with name aps2013105i53.jpg H H graphic file with name aps2013105i54.jpg 7.097 1.67
53 graphic file with name aps2013105i55.jpg H H graphic file with name aps2013105i56.jpg 7.287 1.607
54 graphic file with name aps2013105i57.jpg H H graphic file with name aps2013105i58.jpg 7.232 1.602
55 graphic file with name aps2013105i59.jpg H H graphic file with name aps2013105i60.jpg 6.737 1.417
56 graphic file with name aps2013105i61.jpg H H graphic file with name aps2013105i62.jpg 6.421 1.111
57 graphic file with name aps2013105i63.jpg H H e4rInline graphic 6.904 1.167