Enzymatic inhibitory
(IC50, µM)
Cell growth inhibitory
(IC50, µM)
  R1 R2 R3 EGFRb VEGR-2 PC3a HT29a MCF7a
vandetanib 2-F,4-Br H 0.80 0.07 7.3 1.8 9.6
PD153035 3-Br H CH3 0.0005 0.42 >10 >10 >10
19 NH2 CH3 1.80 >10 >10 3.7 ±0.78 6.0 ±1.67
1 3-Br,4-CH3 H CH3 0.56 >10 >10 >10 >10
20 NH2 CH3 2.64 >10 4.8 ±1.20 3.1 ±0.89 3.6 ±0.62
2 3-Cl,4-F H CH3 0.40 5.30 6.6 ±1.70 6.7 ±0.78 4.9 ±0.54
21 NH2 CH3 0.13 >10 >10 6.2 ±0.28 4.6 ±0.55
3 4-NHCOOCH3 H CH3 6.90 5.80 >10 >10 >10
22 NH2 CH3 >10 >10 7.6 ±0.57 7.1 ±0.61 8.6 ±0.95
4 3-CH3,4-NHCOOC2H5 H CH3 0.90 0.65 >10 >10 >10
23 NH2 CH3 >10 >10 >10 7.2 ±0.71 7.0 ±0.91
5 3-Cl,4-NHCOOC2H5 H CH3 1.00 0.50 9.8 ±0.35 >10 >10
24 NH2 CH3 >10 >10 6.0 ±1.25 3.6 ±2.51 2.0±0.30
aThe cell growth rate was evaluated by performing the MTS assay. Data are represented as the mean ± SEM of at three experiments performed in triplicate. Higher concentrations were not used to avoid precipitation of the compound in the culture medium
bInhibition of EGFR (purified from human arcinoma A431 cells) tyrosine kinase activity
cInhibition of VEGFR-2 (recombinant protein) tyrosine kinase activity
Table 2: Enzymatic and cell growth inhibition results of 2-aminoquinazoline derivatives.