Table 1.
Cpd code | R | MW | Cytotoxicity (IC50a, µM)/cell linesb |
||
---|---|---|---|---|---|
SW620 | PC3 | NCI-H23 | |||
4a | H | 387.87 | 2.09 ± 0.138 | 2.97 ± 0.017 | 1.67 ± 0.056 |
4b | 2-Cl | 422.31 | 0.16 ± 0.002 | 0.16 ± 0.006 | 0.12 ± 0.002 |
4c | 3-Cl | 422.31 | 5.25 ± 0.059 | 4.70 ± 0.145 | 4.81 ± 0.098 |
4d | 4-Cl | 422.31 | 0.002 ± 0.000 | 0.002 ± 0.000 | 0.001 ± 0.000 |
4e | 2,6-Cl2 | 456.75 | >10 | >10 | >10 |
4f | 4-NO2 | 432.86 | 0.011 ± 0.001 | 0.010 ± 0.000 | 0.005 ± 0.001 |
4g | 2-OH | 403.87 | 0.62 ± 0.003 | 0.58 ± 0.014 | 0.69 ± 0.017 |
4h | 2-OH-3-allyl | 443.93 | 0.58 ± 0.000 | 0.61 ± 0.003 | 0.56 ± 0.000 |
4i | 2-OH-4-OCH3 | 433.89 | 0.80 ± 0.042 | 0.83 ± 0.020 | 0.62 ± 0.029 |
4j | 3-OH-4-OCH3 | 433.89 | 5.00 ± 0.065 | 7.31 ± 0.423 | 6.60 ± 0.407 |
4k | 4-OCH3 | 417.89 | 2.53 ± 0.055 | 3.29 ± 0.023 | 2.45 ± 0.028 |
4l | 4-N(CH3)2 | 430.94 | >10 | >10 | >10 |
4m | 3,4,5-(OCH3)3 | 477.94 | >10 | >10 | >10 |
5a | H | 428.88 | 1.96 ± 0.055 | 1.54 ± 0.020 | 1.71 ± 0.044 |
5b | 5-F | 446.87 | 2.28 ± 0.084 | 1.58 ± 0.012 | 1.71 ± 0.040 |
5c | 5-Cl | 463.32 | 4.33 ± 0.223 | 4.46 ± 0.039 | 3.83 ± 0.247 |
5d | 7-Cl | 463.32 | 4.49 ± 0.203 | 3.74 ± 0.142 | 2.68 ± 0.225 |
5e | 5-Br | 507.77 | 1.70 ± 0.051 | 1.61 ± 0.022 | 1.17 ± 0.076 |
5f | 5-CH3 | 442.90 | 7.56 ± 0.200 | 4.71 ± 0.006 | 5.13 ± 0.382 |
5g | 5-OCH3 | 458.90 | 5.27 ± 0.192 | 3.79 ± 0.180 | 3.86 ± 0.076 |
5-FUc | 130.08 | 8.84 ± 1.92 | 13.61 ± 0.46 | 13.45 ± 3.92 | |
PAC-1d | 392.49 | 4.57 ± 0.17 | 4.23 ± 0.45 | 5.11 ± 0.07 | |
Oncrasin-1e | 269.06 | 3.17 ± 0.24 | 3.11 ± 0.28 | 3.32 ± 0.31 |
aThe concentration (µM) of compounds that produces a 50% reduction in cell growth, the numbers represent the averaged results from triplicate experiments with deviation of less than 10%.
bCell lines: SW620, colon cancer; PC3, prostate cancer; NCI-H23, lung cancer.
c5-FU: 5-fluorouracil, a positive control.
dPAC-1: a positive control.
eOncrasin-1: a positive control.