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. 2022 Jan 8;26(5):2595–2612. doi: 10.1007/s11030-021-10347-8

Table 2.

Antiproliferative screening of anthranilamides 1–19 toward human cancer cell lines

Cmpd Structural formula IC50 (µM)a
LN-229 Capan-1 HCT-116 NCI-H460 DND-41 HL-60 K-562 Z-138 HEL 299
1 graphic file with name 11030_2021_10347_Figb_HTML.gif 53.5 ± 12.2 57.6 ± 14.6 > 100 > 100 > 100 > 100 55.7 ± 10.0 > 100 8.0 ± 4.4
2 graphic file with name 11030_2021_10347_Figc_HTML.gif 30.1 ± 2.1 20.4 ± 9.0 32.4 ± 20.0 21.2 ± 10.0 46.2 ± 1.9 41.5 ± 17.0 54.5 ± 18.5 28.6 ± 14.6 > 100
3 graphic file with name 11030_2021_10347_Figd_HTML.gif 48.4 ± 20.0 40.6 ± 4.2 66.1 ± 30.0 69.3 ± 30.7 51.3 ± 4.4 60.5 ± 17.0 51.2 ± 9.3 55.2 ± 9.2 > 100
4 graphic file with name 11030_2021_10347_Fige_HTML.gif > 100 > 100 > 100 > 100 > 100 > 100 > 100 > 100 > 100
5 graphic file with name 11030_2021_10347_Figf_HTML.gif > 100 > 100 > 100 > 100 > 100 > 100 > 100 > 100 > 100
6 graphic file with name 11030_2021_10347_Figg_HTML.gif > 100 > 100 > 100 > 100 > 100 > 100 > 100 > 100 > 100
7 graphic file with name 11030_2021_10347_Figh_HTML.gif 35.8 ± 9.3 27.5 ± 8.1 34.6 ± 6.0 28.4 ± 4.0 53.5 ± 6.7 66.2 ± 18.3 90.7 ± 18.5 21.0 ± 10.1 50.9 ± 2.7
8 graphic file with name 11030_2021_10347_Figi_HTML.gif 20.8 ± 13.8 6.5 ± 2.9 28.9 ± 24.1 8.3 ± 4.3 32.1 ± 20.8 6.7 ± 0.2 29.1 ± 21.3 8.2 ± 1.9 7.1 ± 1.8
9 graphic file with name 11030_2021_10347_Figj_HTML.gif 8.3 ± 3.1 5.8 ± 3.0 32.9 ± 7.9 3.2 ± 1.8 12.5 ± 6.9 10.8 ± 3.3 63.1 ± 36.9 4.1 ± 1.8 7.5 ± 1.0
10 graphic file with name 11030_2021_10347_Figk_HTML.gif 3.0 ± 2.0 4.2 ± 3.4 7.4 ± 1.5 2.2 ± 0.8 8.0 ± 3.2 14.9 ± 7.3 5.9 ± 3.5 4.6 ± 2.0 33.6 ± 15.6
11 graphic file with name 11030_2021_10347_Figl_HTML.gif 39.7 ± 4.4 62.2 ± 9.7 45.4 ± 4.9 87.4 ± 12.6 59.6 ± 1.7 44.7 ± 11.0 18.7 ± 6.7 31.2 ± 1.1 41.6 ± 1.2
12 graphic file with name 11030_2021_10347_Figm_HTML.gif 2.8 ± 1.2 6.3 ± 2.8 8.9 ± 3.0 7.3 ± 1.5 9.2 ± 2.2 9.8 ± 3.5 8.4 ± 3.2 7.2 ± 2.6 7.4 ± 1.2
13 graphic file with name 11030_2021_10347_Fign_HTML.gif 3.1 ± 0.8 5.4 ± 1.8 7.0 ± 0.3 5.3 ± 0.4 7.8 ± 4.1 10.3 ± 3.2 7.7 ± 1.1 6.0 ± 2.6 7.8 ± 1.8
14 graphic file with name 11030_2021_10347_Figo_HTML.gif > 100 > 100 > 100 76.7 ± 25.0 > 100 > 100 > 100 > 100 > 100
15 graphic file with name 11030_2021_10347_Figp_HTML.gif > 100 > 100 > 100 > 100 > 100 > 100 > 100 > 100 > 100
16 graphic file with name 11030_2021_10347_Figq_HTML.gif > 100 > 100 > 100 > 100 > 100 > 100 > 100 > 100 > 100
17 graphic file with name 11030_2021_10347_Figr_HTML.gif 41.0 ± 0.3 31.4 ± 1.9 48.4 ± 3.8 54.8 ± 5.9 61.5 ± 2.1 44.0 ± 8.4 52.0 ± 5.3 35.1 ± 4.5 32.8 ± 3.3
18 graphic file with name 11030_2021_10347_Figs_HTML.gif 44.0 ± 7.6 56.3 ± 24.1 55.0 ± 17.7 43.8 ± 8.4 > 100 > 100 > 100 > 100 > 100
19 graphic file with name 11030_2021_10347_Figt_HTML.gif 46.2 ± 7.5 38.9 ± 5.8 60.8 ± 31.0 55.0 ± 5.0 68.3 ± 12.2 66.3 ± 34.0 64.9 ± 4.9 55.5 ± 12.1 82.6 ± 17.4
CQ 8.9 ± 2.3 46.1 ± 1.3 65.5 ± 7.3 > 100 59.5 ± 3.5 > 100 50.6 ± 2.9 47.4 ± 5.3 84.7 ± 15.3
PQ 45.4 ± 1.2 45.6 ± 3.5 53.9 ± 4.2 > 100 50.2 ± 16.7 28.4 ± 1.6 40.5 ± 6.0 11.4 ± 1.1 > 100
HA > 100 68.6 ± 3.4 > 100 85.1 ± 14.8 > 100 > 100 > 100 57.4 ± 32.6 > 100
DTXb 1.8 ± 3.0 10.0 ± 3.0 2.5 ± 3.0 27.1 ± 3.0 5.5 ± 3.0 13.7 ± 3.0 8.9 ± 3.0 2.5 ± 3.0 nt
STSb 51.1 ± 3.0 38.2 ± 3.0 68.7 ± 3.0 38.4 ± 3.0 40.7 ± 3.0 59.8 ± 3.0 73.9 ± 3.0 40.7 ± 3.0 nt

aIC50, the concentration required to decrease viability or cell growth by 50%; CQ, chloroquine, PQ, primaquine; HA, aminoharmane, DTX, docetaxel, STS, staurosporine

bConcentration in nM