Enzymatic inhibition
(IC50, µM)
Cell growth inhibition
(IC50, µM)
  R EGFRb VEGFR-2c PC3a HT29a MCF7a
PD153035 3-Br 0.0005 0.42 >10 >10 >10
1 3-Br,4-CH3 0.56 >10 >10 >10 >10
2 3-Cl,4-F 0.40 5.30 6.6 ±1.70 6.7 ±0.78 4.9 ±0.54
3 4-NHCOOCH3 6.90 5.80 >10 >10 >10
4 3-CH3,4-NHCOOC2H5 0.90 0.65 >10 >10 >10
5 3-Cl,4-NHCOOC2H5 1.00 0.50 9.8 ±0.35 >10 >10
a The 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 carcinoma A431 cells) tyrosine kinase activity
cInhibition of VEGFR-2 (recombinant protein) tyrosine kinase activity
Table 1: Enzymatic and cell growth inhibition results of quinazoline derivatives.