Table 1.
The IC50 values (μM) of β-carboline monomers (4A, 4B, 4C, and 4D) and bivalent β-carboline derivatives (6a-6f, 6g-6l, 6m-6r, and 6s-6x) against A549, SGC-7901, Hela, SMMC-7721, MCF-7, and MRC5 cell lines.
| Compounds | Substituents | IC50 (μM) Mean ± SD a | ||||||
|---|---|---|---|---|---|---|---|---|
| R1 | R2 | A549 b | SGC-7901 b | Hela b | SMMC-7721 b | MCF-7 b | MRC5 | |
| 4A |
|
- | >80 | >80 | >80 | >80 | >80 | 35.60 ± 0.30 |
| 4B |
|
- | 39.20 ± 1.18 | 42.31 ± 2.13 | 31.28 ± 2.33 | >80 | >80 | 51.78 ± 0.10 |
| 4C |
|
- | 28.06 ± 0.13 | 47.98 ± 0.09 | 42.55 ± 0.98 | >80 | >80 | 35.35 ± 0.30 |
| 4D |
|
- | 13.94 ± 0.07 | 17.84 ± 0.66 | 26.36 ± 1.33 | 35.61 ± 1.33 | 53.92 ± 2.02 | 35.38 ± 0.01 |
| 6a |
|
-(CH2)3- | 24.27 ± 0.12 | 17.76 ± 0.17 | 17.89 ± 0.03 | 25.73 ± 0.32 | 73.45 ± 0.88 | 32.57 ± 0.10 |
| 6b |
|
-(CH2)4- | 12.26 ± 0.04 | 15.48 ± 0.32 | 18.22 ± 0.52 | 66.53 ± 0.31 | 70.88 ± 2.33 | 64.44 ± 0.09 |
| 6c |
|
-(CH2)5- | 17.65 ± 0.09 | 18.72 ± 0.07 | 18.15 ± 0.03 | 55.15 ± 0.03 | 76.85 ± 3.01 | 39.34 ± 0.11 |
| 6d |
|
-(CH2)6- | 40.03 ± 0.15 | 58.41 ± 0.72 | 32.36 ± 0.02 | 33.49 ± 0.01 | 75.47 ± 2.32 | 66.99 ± 0.10 |
| 6e |
|
-(CH2)8- | 50.32 ± 3.15 | 69.97 ± 0.13 | 53.97 ± 0.56 | 75.36 ± 0.89 | >80 | >100 |
| 6f |
|
-CH2-C6H4-CH2- | 29.04 ± 0.06 | 51.24 ± 3.22 | 66.3 ± 1.02 | 57.35 ± 1.13 | >80 | >100 |
| 6g |
|
-(CH2)3- | 18.33 ± 0.28 | 29.42 ± 1.03 | 17.99 ± 0.15 | 73.49 ± 8.06 | 53.14 ± 2.28 | 32.61 ± 0.10 |
| 6h |
|
-(CH2)4- | 8.09 ± 0.25 | 17.75 ± 0.93 | 45.75 ± 0.55 | 24.71 ± 0.5 | 76.73 ± 5.0 | 50.78 ± 0.09 |
| 6i |
|
-(CH2)5- | 6.93 ± 0.33 | 7.18 ± 0.01 | 9.88 ± 0.04 | 14.22 ± 0.28 | 59.29 ± 5.86 | 37.99 ± 0.10 |
| 6j |
|
-(CH2)6- | 12.18 ± 0.06 | 26.26 ± 1.03 | 18.05 ± 1.03 | 16.68 ± 0.03 | 64.49 ± 3.31 | 41.0 ± 0.07 |
| 6k |
|
-(CH2)8- | 37.36 ± 2.08 | 35.00 ± 2.09 | 36.69 ± 2.02 | 33.93 ± 0.52 | 44.93 ± 2.99 | 65.85 ± 0.07 |
| 6l |
|
-CH2-C6H4-CH2- | 30.13 ± 0.37 | 39.26 ± 1.22 | 59.68 ± 1.52 | 69.66 ± 0.30 | 70.76 ± 2.02 | 37.66 ± 0.13 |
| 6m |
|
-(CH2)3- | 19.84 ± 0.04 | 18.41 ± 0.31 | 17.95 ± 0.02 | 33.32 ± 0.03 | 28.43 ± 0.28 | 49.05 ± 0.12 |
| 6n |
|
-(CH2)4- | 13.36 ± 0.35 | 37.79 ± 1.02 | 27.96 ± 0.99 | 42.72 ± 2.18 | 49.06 ± 2.23 | 26.39 ± 0.01 |
| 6o |
|
-(CH2)5- | 11.23 ± 0.61 | 17.18 ± 0.03 | 18.76 ± 0.46 | 36.62 ± 0.12 | 49.37 ± 1.65 | 31.28±0.07 |
| 6p |
|
-(CH2)6- | 19.28 ± 0.02 | 17.84 ± 0.22 | 15.66 ± 0.33 | 26.75 ± 0.51 | 55.04 ± 2.22 | 47.60 ± 0.02 |
| 6q |
|
-(CH2)8- | 23.65 ± 0.05 | 35.78 ± 0.82 | 45.21 ± 1.66 | 29.82 ± 0.93 | 43.05 ± 2.01 | 42.06 ± 0.09 |
| 6r |
|
-CH2-C6H4-CH2- | 46.61 ± 0.03 | 65.93 ± 1.18 | 58.25 ± 2.98 | >80 | 68.26 ± 1.25 | 56.11 ± 0.01 |
| 6s |
|
-(CH2)3- | 6.12 ± 0.03 | 8.06 ± 0.08 | 13.77 ± 0.11 | 14.71 ± 0.08 | 25.20 ± 1.12 | 22.82 ± 0.02 |
| 6t |
|
-(CH2)4- | 12.39 ± 0.59 | 9.01 ± 0.19 | 15.20 ± 0.32 | 18.26 ± 0.18 | 25.69 ± 1.21 | >100 |
| 6u |
|
-(CH2)5- | 5.61 ± 0.04 | 5.86 ± 0.08 | 14.63 ± 0.36 | 16.68 ± 0.11 | 36.03 ± 2.99 | 39.89 ± 0.05 |
| 6v |
|
-(CH2)6- | 7.95 ± 0.06 | 8.60 ± 0.13 | 22.85 ± 1.36 | 24.65 ± 0.06 | 42.41 ± 2.08 | 67.75 ± 0.11 |
| 6w |
|
-(CH2)8- | 16.54 ± 0.33 | 29.98 ± 0.07 | 31.34 ± 1.88 | 44.57 ± 0.02 | 76.32 ± 3.36 | 60.78 ± 0.16 |
| 6x |
|
-CH2-C6H4-CH2- | 34.27 ± 0.05 | 45.00 ± 0.16 | 39.61 ± 2.59 | >80 | >80 | 63.28 ± 0.10 |
| 5-FU c | C4H3FN2O2 | 15.39 ± 0.09 | >80 | >80 | 52.32 ± 2.06 | 57.69 ± 1.39 | 16.33 ± 0.30 | |
a IC50 was the concentration when cell viability was reduced by 50% after treatment with β-carbolines for 48 h, and all data were the mean values of three independent experiments. b A549: lung carcinoma, SGC-7901: gastric carcinoma, Hela: cervical carcinoma, SMMC-7721: liver carcinoma, MCF-7: breast carcinoma, MRC5: normal lung cell. c 5-FU (5-fluorouracil, which could insert into DNA, interfering with DNA synthesis) was used as a positive control.