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. 2023 May 29;24(11):9450. doi: 10.3390/ijms24119450

Table 23.

Antiproliferative activities of thiazolo[5,4-b]pyridine derivatives.

Compd. GI50 (µM) a Entry GI50 (µM) a
GIST-T1 HMC1.2 GIST-T1 HMC1.2
imatinib 0.02 ± 0.01 27.10 ± 3.36 142p 0.66 ± 0.10 8.55 ± 2.40
sunitinib 0.01 ± 0.00 2.53 ± 0.35 142q 0.42 ± 0.07 15.53 ± 3.97
142a >50 Inactive b 142r 0.01 ± 0.00 1.15 ± 0.96
142b 33.05 ± 7.09 Inactive b 142s 0.02 ± 0.00 1.33 ± 0.43
142c 33.69 ± 3.45 Inactive b 142t 0.12 ± 0.03 6.62 ± 0.75
142d 16.36 ± 2.73 25.18 ± 2.21 142u 0.66 ± 0.08 11.31 ± 0.34
142e 3.45 ± 0.41 11.53 ± 0.62 142v 0.05 ± 0.01 6.81 ± 0.67
142f 20.94 ± 2.00 Inactive b 142w 0.02 ± 0.01 4.99 ± 0.43
142g 10.84 ± 1.06 36.77 ± 10.9 143a 0.08 ± 0.01 4.58 ± 0.32
142h 0.96 ± 0.10 7.26 ± 4.13 143b 0.10 ± 0.01 5.22 ± 0.59
142i 7.16 ± 0.87 9.65 ± 1.06 143c 0.01 ± 0.00 1.52 ± 0.43
142j 3.31 ± 0.73 6.35 ± 0.32 143d 8.13 ±1.81 Inactive b
142k 0.18 ± 0.03 2.27 ± 0.84 143e 0.23 ± 0.07 14.04 ± 10.2
142l 0.08 ± 0.01 4.34 ± 1.31 143f 0.30 ± 0.06 28.39 ± 13.3
142m 0.27 ± 0.17 3.41 ± 1.49 143g 0.07 ± 0.01 4.88 ± 1.18
142n 0.55 ± 0.09 7.00 ± 2.68 143h 0.02 ± 0.00 4.98 ± 0.32
142o 0.28 ± 0.08 2.36 ± 0.58

a Radiometric biochemical kinase assay results. b less than 50% inhibition at a concentration of 10 µM.