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. 2022 Aug 23;37(1):2265–2282. doi: 10.1080/14756366.2022.2104841

Table 1.

EGFR and VEGFR-2 kinases inhibitory activity of target thiazolyl-pyrazoline derivatives.

graphic file with name IENZ_A_2104841_ILG0001_C.jpg

Compound R R1 IC50 (nM) ± SEM
EGFR VEGFR-2
7a H H 145.1 ± 2.0 124.9 ± 1.4
7b H Cl 114.2 ± 0.4 195.2 ± 4.6
7c OCH3 H 511.2 ± 3.2 915.2 ± 4.3
7d OCH3 Cl 132.9 ± 1.2 185.5 ± 2.3
10a H CH3 274.0 ± 2.3 450.3 ± 8.3
10b H OCH2CH3 40.7 ± 1.0 78.4 ± 1.5
10c H NHC6H5 130.7 ± 1.1 102.2 ± 4.3
10d OCH3 NHC6H5 32.5 ± 2.2 43.0 ± 2.4
13a H H 973.0 ± 2.0 1151.2 ± 4.3
13b H CH3 179.4 ± 0.0 214.3 ± 4.0
13c H Cl 134.5 ± 1.5 173.3 ± 2.6
13d OCH3 H 93.6 ± 3.0 335.8 ± 6.3
13e OCH3 CH3 67.7 ± 2.0 216.4 ± 4.3
13f OCH3 Cl 107.13 ± 1.2 113.3 ± 1.8
Gefitinib 55.74 ± 1.0 45.3 ± 1.2
Vandetanib 43.14 ± 1.3 29.1 ± 1.0