From: Design, synthesis and biological evaluation of novel betulinic acid derivatives
Compound | IC50 (μM) a values against five human carcinoma cells | ||||
---|---|---|---|---|---|
MGC-803b | PC3c | A375d | Bcap-37e | A431f | |
1 | 41.2 ± 0.6 | 67.2 ± 0.5 | > 100 | > 100 | 15.7 ± 0.2 |
2a | > 20 | > 20 | > 20 | > 20 | > 20 |
2b | > 20 | > 20 | > 20 | > 20 | > 20 |
2c | > 20 | > 20 | > 20 | > 20 | > 20 |
3a | 3.5 ± 0.5 | 5.6 ± 0.9 | 3.4 ± 0.1 | 5.5 ± 0.8 | 4.8 ± 0.2 |
3b | 3.4 ± 0.2 | 4.2 ± 0.2 | 6.0 ± 0.4 | 7.6 ± 0.5 | 5.7 ± 0.2 |
3c | 2.3 ± 0.2 | 4.6 ± 0.5 | 3.3 ± 0.4 | 3.6 ± 1.2 | 4.3 ± 0.3 |
3d | 7.6 ± 2.1 | 8.6 ± 0.2 | 12.4 ± 1.1 | 10.5 ± 0.5 | 11.8 ± 0.6 |
3e | 4.0 ± 0.9 | 3.8 ± 1.1 | 4.4 ± 0.5 | 3.0 ± 1.1 | 5.6 ± 0.1 |
3f | 4.3 ± 0.2 | 2.8 ± 0.4 | 2.7 ± 0.3 | 5.2 ± 0.1 | 3.5 ± 0.6 |
3g | 15.7 ± 0.5 | 13.4 ± 0.9 | 11.3 ± 0.6 | 16.2 ± 0.5 | 13.3 ± 0.4 |
3h | 12.7 ± 1.2 | 15.0 ± 0.5 | 11.6 ± 0.5 | 12.5 ± 0.5 | 9.6 ± 0.9 |
3i | 5.6 ± 0.4 | 7.9 ± 0.5 | 7.7 ± 0.3 | 6.8 ± 1.2 | 5.7 ± 0.2 |
3j | 7.6 ± 0.6 | 13.4 ± 0.7 | 12.8 ± 0.4 | 7.5 ± 0.6 | 10.5 ± 1.5 |
3k | 16.7 ± 0.5 | 17.1 ± 0.2 | > 20 | > 20 | 15.7 ± 0.7 |
3l | 11.8 ± 0.3 | 12.7 ± 1.5 | 13.9 ± 0.8 | 9.43 ± 0.8 | 7.0 ± 0.4 |
5a | 8.8 ± 0.8 | 10.1 ± 0.5 | 12.5 ± 0.6 | 9.4 ± 0.7 | 6.3 ± 0.8 |
5b | 13.4 ± 0.1 | 14.5 ± 0.4 | 15.3 ± 2.3 | 16.7 ± 0.8 | 12.9 ± 1.2 |
5c | 17.3 ± 0.4 | > 20 | > 20 | > 20 | > 20 |
5d | > 20 | 18.9 ± 0.3 | > 20 | > 20 | 16.3 ± 0.1 |
5e | > 20 | > 20 | > 20 | > 20 | > 20 |
5f | 15.4 ± 0.6 | > 20 | > 20 | > 20 | > 20 |
HCPT | 29.1 ± 2.6 | 34.5 ± 1.5 | 27.8 ± 1.2 | 28.1 ± 1.0 | 23.4 ± 0.7 |
ADM | 0.7 ± 0.2 | 0.6 ± 0.1 | 1.0 ± 0.6 | 1.2 ± 0.2 | 1.1 ± 0.1 |