Table 2.
Structure and biological activity of pyrrolo[2,3‐d]pyrimidine derivatives 2 a–q.
|
|
|
|
|
|
|
|
|
|
|---|---|---|---|---|---|---|---|---|
|
Entry |
Compound |
R |
R′ |
Pf 3D7 % cell viability at 20 μM[a] |
Pf 3D7 IC50 [μM][b] |
Pf CDPK1 IC50 [μM]0[b] |
Pf CDPK4 IC50 [μM][b] |
Hela % cell viability at 20 μM[a] |
|
1 |
2 a |
|
|
103.0±8.0 |
– |
– |
– |
93.6±7.1 |
|
2 |
2 b |
|
|
24.1±3.8 |
18.7±0.8 |
>2 |
0.3694±0.1381 |
79.8±3.3 |
|
3 |
2 c |
|
|
93.1±1.4 |
– |
– |
– |
73±4.1 |
|
4 |
2 d |
|
|
106.6±6.0 |
– |
>2 |
>2 |
63.8±1.5 |
|
5 |
2 e |
|
|
110.2±10.9 |
– |
0.5885±0.2059 |
>2 |
88.8±0.7 |
|
6 |
2 f |
|
|
35.3±2.2 |
– |
>2 |
0.2104±0.0680 |
92.1±3.1 |
|
7 |
2 g |
|
|
9.3±1.6 |
14.2±1.7 |
>2 |
0.5298±0.1847 |
92.8±5.7 |
|
8 |
2 h |
|
|
62.2±9.0 |
– |
>2 |
>2 |
94.4±9.3 |
|
9 |
2 i |
|
|
121.4±8.6 |
– |
>2 |
>2 |
93.3±3.2 |
|
10 |
2 j |
|
|
2.8±3.9 |
12.1±11.4 |
>2 |
>2 |
79.3±0.8 |
|
14 |
2 k |
|
|
62.0±2.1 |
– |
– |
– |
78.9±0.1 |
|
15 |
2 l |
|
|
66.8±3.9 |
– |
>2 |
>2 |
82.4±1.4 |
|
16 |
2 m |
|
|
12.0±2.6 |
8.2±3.1 |
– |
– |
47.0±7.0 |
|
17 |
2 n |
|
|
95.0±1.0 |
– |
>2 |
>2 |
112.0±2.8 |
|
18 |
2 o |
|
|
57.0±6.6 |
– |
>2 |
>2 |
88.0±11.8 |
|
19 |
2 p |
|
|
72.4±13.3 |
– |
– |
– |
97.0±12.5 |
|
20 |
2 q |
|
|
110.0±4.2 |
– |
– |
– |
95.4±0.5 |
|
21 |
Chloroquine |
|
|
– |
0.015 |
– |
– |
– |
[a] Data are presented as the mean ±SD of two replicates. [b] Data are presented as the mean ±SD of three replicates.