Table 1.
| ||||||||
---|---|---|---|---|---|---|---|---|
IC50
a
(µM) |
||||||||
Compounds | Purine or pseudopurine | R | A549 | CFPAC-1 | HeLa | SW620 | WI38/HFF-1 b | ClogP c |
4a | 53.22 | 33.39 | 34.21 | 38.94 | 5.21 | 2.68 | ||
4c | 15.91 | 7.90 | 12.30 | 14.69 | 0.75 | 3.44 | ||
4d | 54.65 | 31.10 | 33.21 | 41.75 | 23.88 | 2.68 | ||
4e | 88.95 | >100 | 57.96 | 92.50 | 6.58 | 1.68 | ||
5c | 9.43 | 7.39 | 22.52 | 11.77 | 5.21 | 3.29 | ||
5d | 73.86 | >100 | >100 | 90.25 | 23.89 | 2.53 | ||
5e | >100 | >100 | >100 | >100 | 60.49 | 1.53 | ||
6e | >100 | >100 | >100 | >100 | 73.63 | 2.14 | ||
7c | >100 | 89.24 | 36.80 | 68.95 | 19.43 | 3.29 | ||
7e | >100 | >100 | 8.77 | >100 | 7.62 | 1.53 | ||
8a | 85.36 | 48.37 | 39.41 | 8.50 | 32.18 | 3.44 | ||
8b | 64.52 | 47.69 | 65.46 | 44.64 | 21.02 | 3.84 | ||
8c | 46.91 | 46.55 | 38.83 | 37.05 | 4.62 | 4.20 | ||
8d | 69.02 | 35.19 | 83.32 | 65.45 | 22.53 | 3.44 | ||
8e | 69.19 | 36.27 | 33.59 | 73.48 | 39.93 | 2.44 | ||
9c | 66.36 | 62.77 | 32.89 | 55.74 | 57.54 | 5.03 | ||
9d | 86.36 | 65.10 | 20.03 | 65.90 | 48.47 | 4.27 | ||
9e | 45.45 | 47.30 | 24.50 | 45.09 | 10.78 | 3.27 | ||
10a | >100 | >100 | >100 | >100 | >100 | 3.89 | ||
10b | 40.16 | >100 | 31.01 | 45.84 | 58.07 | 4.29 | ||
10c | 71.57 | 64.71 | 53.01 | 54.25 | 24.03 | 4.65 | ||
10d | >100 | >100 | 82.92 | >100 | >100 | 3.89 | ||
10e | 51.93 | 77.08 | 47.63 | 57.55 | 45.70 | 2.89 | ||
11a | 44.01 | >100 | >100 | 43.29 | >100 b | 3.95 | ||
11b | >100 | >100 | >100 | >100 | >100 b | 4.41 | ||
11c | >100 | >100 | >100 | >100 | >100 b | 4.68 | ||
11d | 51.27 | 85.56 | 71.15 | 44.83 | 40.42 b | 3.95 | ||
11e | 75.38 | >100 | 83.01 | 68.49 | 40.00 b | 3.17 | ||
12a | 76.26 | 86.52 | 71.70 | 99.92 | 91.91 | 3.14 | ||
12b | 0.79 | 52.55 | 42.17 | 91.23 | 38.10 | 3.60 | ||
12c | 14.18 | 56.43 | 30.61 | >100 | >100 | 3.87 | ||
12d | 36.25 | 34.68 | 21.94 | >100 | 30.63 | 3.14 | ||
12e | >100 | >100 | >100 | >100 | >100 | 2.35 |
50% inhibitory concentration or compound concentration required inhibiting tumour cell proliferation by 50%.
Compounds 11a–e were tested in HFF-1 cell line.
Values of n-octanol/water partition coefficients logP were calculated using ChemAxon algorithm (MarvinView Ver. 6.2.2.).