
Entry |
Comp. |
X |
R1 |
R2 |
EC50b (μM) |
CC50c (μM) |
TId |
1 |
5a |
CH2 |
Ph |
OEt |
63.37 |
234.02 |
3.69 |
2 |
5b |
CH2 |
2-FPh |
OEt |
252.56 |
>581.40 |
>2.30 |
3 |
5c |
CH2 |
4-FPh |
OEt |
88.89 |
323.32 |
3.64 |
4 |
5d |
CH2 |
2-OMePh |
OEt |
57.58 |
395.39 |
6.87 |
5 |
5e |
CH2 |
3-OMePh |
OEt |
213.17 |
>561.80 |
>2.64 |
6 |
5f |
CH2 |
4-OMePh |
OEt |
69.18 |
243.69 |
3.52 |
7 |
5g |
CH2 |
3,4-OMePh |
OEt |
288.91 |
>518.13 |
>1.79 |
8 |
5h |
CH2 |
naphthalen-1-yl |
OEt |
48.32 |
>531.91 |
>11.01 |
9 |
5i |
CH(CH3) |
Ph |
OEt |
68.79 |
320.09 |
4.65 |
10 |
6a |
NH |
4-FPh |
OEt |
32.61 |
213.01 |
6.53 |
11 |
6b |
NH |
4-ClPh |
OEt |
14.59 |
135.46 |
9.28 |
12 |
7a |
CH2CH2 |
Ph |
OEt |
55.91 |
376.18 |
6.73 |
13 |
7b |
CH2CH2 |
2-FPh |
OEt |
44.83 |
148.80 |
3.32 |
14 |
7c |
CH2CH2 |
3-FPh |
OEt |
52.26 |
176.42 |
3.38 |
15 |
7d |
CH2CH2 |
4-FPh |
OEt |
1.65 |
13.16 |
7.98 |
16 |
7e |
CH2CH2 |
4-ClPh |
OEt |
15.16 |
145.43 |
9.59 |
17 |
7f |
CH2CH2 |
4-MePh |
OEt |
2.34 |
15.45 |
6.60 |
18 |
7g |
CH2CH2 |
4-SO2NH2 |
OEt |
136.42 |
173.46 |
1.27 |
19 |
7h |
CH2CH2 |
4-OMePh |
OEt |
163.92 |
232.97 |
1.42 |
20 |
7i |
CH2CH2 |
3,4-OMePh |
OEt |
9.15 |
33.52 |
3.66 |
21 |
7j |
CH2CH2 |
indol-3-yl |
OEt |
9.37 |
26.73 |
2.85 |
22 |
8a |
CH2CH2 |
4-MePh |
NH(4-FBn) |
40.37 |
164.60 |
4.08 |
23 |
8b |
CH2CH2 |
4-MePh |
NH(2-OMeBn) |
32.70 |
215.82 |
6.60 |
24 |
8c |
CH2CH2 |
4-MePh |
NHCH2CH(CH2CH2) |
36.41 |
306.17 |
8.41 |
25 |
8d |
CH2CH2 |
4-FPh |
NH(4-FBn) |
5.70 |
30.76 |
5.40 |
26 |
8e |
CH2CH2 |
4-FPh |
NH(2-OMeBn) |
63.01 |
224.25 |
3.56 |
27 |
8f |
CH2CH2 |
3,4-OMePh |
NH(2-OMeBn) |
149.25 |
217.70 |
1.46 |
28 |
9a |
CH2CO |
4-BrPh |
OEt |
54.27 |
>464.04 |
>8.55 |
29 |
9b |
CH2CH(CH3) |
Ph |
OEt |
25.14 |
146.10 |
5.81 |
30 |
9c |
CH2CH(Ph) |
Ph |
OEt |
3.10 |
25.22 |
8.14 |
31 |
9d |
CH(COOMe)CH2 |
Ph |
OEt |
185.55 |
346.88 |
1.87 |
32 |
10 |
CH2CH2CH2 |
Ph |
OEt |
59.15 |
206.41 |
3.49 |
33 |
11 |
1,2,3,4-tetrahydronaphthalen-1-yl |
OEt |
36.64 |
132.92 |
3.63 |
34 |
12 |
propyl |
OEt |
352.81 |
>719.42 |
>2.03 |
35 |
13 |
t-butyl |
OEt |
119.38 |
>684.93 |
>5.74 |
36 |
AZTe |
- |
- |
- |
0.0085 |
3779 |
444588 |
|