Table 1.
The growth-inhibition effects in vitro of l-ascorbic acid and compounds 8a−8u on selected tumor cell lines and normal fibroblasts.
| Compd. | R | IC50a/μM |
clogPb | |||||||
|---|---|---|---|---|---|---|---|---|---|---|
| A549 | CFPAC-1 | HCT-116 | HeLa | HepG2 | MCF-7 | SW620 | HFF | |||
| 8a | H | >100 | >100 | >100 | >100 | >100 | >100 | >100 | 0.61± 0.42 |
0.80 |
| 8b | Si(CH3)3 | 19.18± 12.63 |
52.56± 6.35 |
31.81± 0.36 |
22.30± 0.36 |
24.11± 0.37 |
12.13± 10.51 |
56.03± 11.09 |
20.02± 1.07 |
3.16 |
| 8c |  |
28.89± 15.94 |
66.47± 14.92 |
57.19± 43.37 |
35.53± 17.15 |
33.78± 15.04 |
45.89± 21.84 |
49.20± 4.19 |
80.69± 45.52 |
4.25 |
| 8d |  |
41.24± 22.18 |
62.37± 52.22 |
48.24± 61.60 |
40.77± 1.34 |
11.61± 5.52 |
27.73± 30.59 |
>100 | >100 | 2.75 |
| 8e |  |
0.75± 4.26 |
5.83± 0.06 |
9.42± 1.93 |
3.91± 3.04 |
5.07± 2.61 |
5.62± 2.26 |
3.76± 4.64 |
5.10± 6.76 |
3.28 |
| 8f |  |
8.69± 0.05 |
>100 | >100 | 25.47± 66.03 |
8.77± 0.90 |
>100 | >100 | >100 | 2.89 |
| 8g |  |
28.27± 0.24 |
26.02± 9.79 |
>100 | 16.39± 21.05 |
46.43± 17.89 |
99.73± 0.77 |
58.22± 59.57 |
<0.01 | 2.48 |
| 8h |  |
>100 | >100 | >100 | >100 | >100 | >100 | >100 | 0.05± 70.14 |
2.48 |
| 8i |  |
59.94± 7.82 |
54.08± 5.17 |
42.87± 19.40 |
39.26± 17.70 |
62.66± 32.48 |
51.84± 11.29 |
>100 | 39.04± 27.59 |
2.20 |
| 8j |  |
6.22± 1.73 |
9.89± 30.48 |
13.83± 31.97 |
8.39± 1.16 |
7.46± 0.43 |
9.01± 12.40 |
12.18± 8.62 |
>100 | 4.67 |
| 8k |  |
43.85± 9.99 |
47.67± 12.21 |
30.36± 3.18 |
26.52± 19.26 |
38.09± 19.04 |
25.91± 1.51 |
54.22± 17.58 |
24.31± 7.04 |
1.97 |
| 8l |  |
28.56± 34.71 |
73.22± 12.44 |
10.36± 17.35 |
18.07± 21.40 |
32.83± 22.34 |
7.91± 11.42 |
47.53± 1.32 |
26.27± 0.40 |
2.52 |
| 8m |  |
6.75± 24.43 |
40.27± 41.70 |
28.83± 32.21 |
22.89± 20.12 |
12.24± 22.17 |
0.08± 55.51 |
45.15± 2.86 |
>100 | 5.25 |
| 8n |  |
33.97± 13.52 |
54.88± 2.03 |
28.26± 2.22 |
18.33± 11.76 |
29.21± 9.51 |
0.73± 8.48 |
35.78± 6.38 |
13.33± 5.15 |
2.44 |
| 8o |  |
29.00± 20.77 |
58.78± 23.78 |
36.08± 19.22 |
36.66± 11.34 |
34.99± 5.45 |
24.53± 18.57 |
68.50± 4.37 |
27.07± 10.95 |
2.30 |
| 8p |  |
>100 | >100 | 72.69± 7.35 |
68.77± 43.87 |
68.06± 1.73 |
63.37± 2.61 |
>100 | 58.53± 41.44 |
0.69 |
| 8q |  |
16.76± 50.14 |
68.01± 20.79 |
13.09± 22.76 |
14.36± 0.63 |
24.94± 7.80 |
6.40± 11.19 |
45.79± 6.49 |
0.05± 5.63 |
1.74 |
| 8r |  |
2.87± 29.22 |
38.87± 32.64 |
8.38± 0.66 |
13.63± 11.70 |
7.51± 1.60 |
4.17± 24.27 |
18.00± 3.71 |
0.02± 0.03 |
2.00 |
| 8s |  |
39.06± 59.22 |
58.16± 9.96 |
21.61± 13.87 |
20.71± 4.18 |
25.46± 7.57 |
3.39± 14.43 |
42.39± 2.36 |
0.02± 0.02 |
2.10 |
| 8t |  |
22.51± 29.96 |
34.68± 8.04 |
22.90± 2.18 |
24.97± 9.16 |
18.34± 8.31 |
26.81± 11.19 |
41.05± 12.13 |
0.03± 0.04 |
1.50 |
| 8u |  |
>100 | >100 | >100 | >100 | >100 | >100 | >100 | 0.06± 0.14 |
2.84 |
| L-ASA | >100 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | ||
a
50% inhibitory concentration or compound concentration required to inhibit tumor cell proliferation by 50%. NA = not active.
b
Values of clog P were calculated by DataWarrior [36].