TABLE 1.
Compounds | X | R1 | Z | IC50 (μM) a | |||
---|---|---|---|---|---|---|---|
A549 | MCF-7 | Hela | c-Met | ||||
16a | H | H | 12.36 ± 0.97 | 13.76 ± 1.23 | 21.54 ± 1.78 | 0.794 | |
16b | H | H | 6.46 ± 0.33 | 7.87 ± 0.42 | 12.16 ± 1.08 | 0.379 | |
16c | H | H | 5.58 ± 0.75 | 6.45 ± 0.81 | 14.31 ± 1.15 | 0.345 | |
16d | H | H | 12.35 ± 0.98 | 11.52 ± 1.06 | 19.53 ± 1.94 | 0.722 | |
16e | H | H | 5.44 ± 0.42 | 7.13 ± 0.63 | 11.19 ± 0.96 | 0.342 | |
16f | H | H | 27.33 ± 0.86 | >50 | >50 | >1 | |
16 g | F | H | 8.21 ± 0.65 | 9.17 ± 1.03 | 17.73 ± 1.29 | 0.658 | |
16 h | F | H | 6.56 ± 0.42 | 8.18 ± 1.12 | 13.94 ± 1.59 | 0.437 | |
16i | F | H | 17.35 ± 0.97 | 19.03 ± 1.32 | 24.96 ± 2.17 | ND b | |
16j | F | H | 3.26 ± 0.67 | 3.68 ± 0.34 | 6.17 ± 0.58 | 0.110 | |
16 k | F | H | 6.18 ± 0.34 | 6.51 ± 0.63 | 12.89 ± 1.06 | 0.380 | |
16l | F | H | 11.44 ± 0.76 | 11.97 ± 1.24 | 23.32 ± 2.12 | 0.725 | |
17a | H | CH3 | 1.23 ± 0.13 | 1.43 ± 0.21 | 2.31 ± 0.29 | 0.055 | |
17b | H | CH3 | 4.31 ± 0.49 | 5.15 ± 0.72 | 9.46 ± 0.58 | 0.245 | |
17c | H | CH3 | 7.68 ± 0.71 | 8.79 ± 0.89 | 15.88 ± 1.10 | 0.532 | |
17d | H | CH3 | 5.21 ± 0.37 | 6.95 ± 0.67 | 10.73 ± 1.42 | 0.289 | |
17e | H | CH3 | 2.05 ± 0.19 | 1.74 ± 0.22 | 4.78 ± 0.43 | 0.077 | |
17f | H | CH3 | 5.73 ± 0.54 | 6.38 ± 0.85 | 12.37 ± 1.53 | 0.300 | |
17 g | F | CH3 | 4.65 ± 0.66 | 4.83 ± 0.33 | 9.25 ± 0.45 | 0.232 | |
17 h | F | CH3 | 3.56 ± 0.32 | 4.25 ± 0.76 | 7.43 ± 0.38 | 0.156 | |
17i | F | CH3 | 188 | 25.44 ± 1.54 | >50 | ND | |
17j | F | CH3 | 7.16 ± 0.45 | 7.31 ± 0.77 | 14.18 ± 1.64 | 0.450 | |
17 k | F | CH3 | 15.34 ± 0.51 | 18.17 ± 1.28 | 25.33 ± 2.40 | ND | |
17l | F | CH3 | 0.98 ± 0.08 | 1.05 ± 0.17 | 1.28 ± 0.25 | 0.026 | |
17 m | F | CH3 | 8.84 ± 0.97 | 9.34 ± 1.03 | 17.37 ± 1.56 | 0.653 | |
Foretinib c | - | - | - | 0.71 ± 0.05 | 0.93 ± 0.09 | 1.18 ± 0.25 | 0.019 |
Note. A549, human lung adenocarcinoma; MCF-7, human breast cancer; Hela, human cervical carcinoma.
The values are the average of two separate determinations.
ND, not detected.
Used as a positive control.