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. 2025 Feb 13. Online ahead of print. doi: 10.1039/d5md00025d

Table 1. Activity of quinoline and isoquinoline derivatives in in vitro kinase and cell-based assays.

graphic file with name d5md00025d-u1.jpg
Compound Structures % inhibition IC50 (nM)
EGFR HER2 SKBR3
1 μM 0.1 μM 1 μM 0.1 μM
4 a–e 90 59 92 62 1358
9a a–f 91 56 92 55 235
9b a–g 98 85 95 58 125
9c a–h 76 32 80 40 3199
9d a–i 59 22 73 30 4527
11a b–d 69 16 91 50 1175
11b b–e 87 33 86 32 725
11c b–f 84 43 77 33 553
12a c–d 68 10 92 56 1389
12b c–e 61 9 88 44 610
12c c–f 66 15 83 37 392
14a c–g 92 54 92 43 103
Lapatinib 99 94 96 70 23