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. 2022 Apr 6;10:815534. doi: 10.3389/fchem.2022.815534

TABLE 1.

Antiproliferative and mesenchymal–epithelial transition factor (c-Met) kinase inhibitory activities of the target compounds.

graphic file with name fchem-10-815534-fx1.jpg
Compounds X R1 Z IC50 (μM) a
A549 MCF-7 Hela c-Met
16a H H graphic file with name fchem-10-815534-fx2.jpg 12.36 ± 0.97 13.76 ± 1.23 21.54 ± 1.78 0.794
16b H H graphic file with name fchem-10-815534-fx3.jpg 6.46 ± 0.33 7.87 ± 0.42 12.16 ± 1.08 0.379
16c H H graphic file with name fchem-10-815534-fx4.jpg 5.58 ± 0.75 6.45 ± 0.81 14.31 ± 1.15 0.345
16d H H graphic file with name fchem-10-815534-fx5.jpg 12.35 ± 0.98 11.52 ± 1.06 19.53 ± 1.94 0.722
16e H H graphic file with name fchem-10-815534-fx6.jpg 5.44 ± 0.42 7.13 ± 0.63 11.19 ± 0.96 0.342
16f H H graphic file with name fchem-10-815534-fx7.jpg 27.33 ± 0.86 >50 >50 >1
16 g F H graphic file with name fchem-10-815534-fx8.jpg 8.21 ± 0.65 9.17 ± 1.03 17.73 ± 1.29 0.658
16 h F H graphic file with name fchem-10-815534-fx9.jpg 6.56 ± 0.42 8.18 ± 1.12 13.94 ± 1.59 0.437
16i F H graphic file with name fchem-10-815534-fx10.jpg 17.35 ± 0.97 19.03 ± 1.32 24.96 ± 2.17 ND b
16j F H graphic file with name fchem-10-815534-fx11.jpg 3.26 ± 0.67 3.68 ± 0.34 6.17 ± 0.58 0.110
16 k F H graphic file with name fchem-10-815534-fx12.jpg 6.18 ± 0.34 6.51 ± 0.63 12.89 ± 1.06 0.380
16l F H graphic file with name fchem-10-815534-fx13.jpg 11.44 ± 0.76 11.97 ± 1.24 23.32 ± 2.12 0.725
17a H CH3 graphic file with name fchem-10-815534-fx14.jpg 1.23 ± 0.13 1.43 ± 0.21 2.31 ± 0.29 0.055
17b H CH3 graphic file with name fchem-10-815534-fx15.jpg 4.31 ± 0.49 5.15 ± 0.72 9.46 ± 0.58 0.245
17c H CH3 graphic file with name fchem-10-815534-fx16.jpg 7.68 ± 0.71 8.79 ± 0.89 15.88 ± 1.10 0.532
17d H CH3 graphic file with name fchem-10-815534-fx17.jpg 5.21 ± 0.37 6.95 ± 0.67 10.73 ± 1.42 0.289
17e H CH3 graphic file with name fchem-10-815534-fx18.jpg 2.05 ± 0.19 1.74 ± 0.22 4.78 ± 0.43 0.077
17f H CH3 graphic file with name fchem-10-815534-fx19.jpg 5.73 ± 0.54 6.38 ± 0.85 12.37 ± 1.53 0.300
17 g F CH3 graphic file with name fchem-10-815534-fx20.jpg 4.65 ± 0.66 4.83 ± 0.33 9.25 ± 0.45 0.232
17 h F CH3 graphic file with name fchem-10-815534-fx21.jpg 3.56 ± 0.32 4.25 ± 0.76 7.43 ± 0.38 0.156
17i F CH3 graphic file with name fchem-10-815534-fx22.jpg 188 25.44 ± 1.54 >50 ND
17j F CH3 graphic file with name fchem-10-815534-fx23.jpg 7.16 ± 0.45 7.31 ± 0.77 14.18 ± 1.64 0.450
17 k F CH3 graphic file with name fchem-10-815534-fx24.jpg 15.34 ± 0.51 18.17 ± 1.28 25.33 ± 2.40 ND
17l F CH3 graphic file with name fchem-10-815534-fx25.jpg 0.98 ± 0.08 1.05 ± 0.17 1.28 ± 0.25 0.026
17 m F CH3 graphic file with name fchem-10-815534-fx26.jpg 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.

a

The values are the average of two separate determinations.

b

ND, not detected.

c

Used as a positive control.