| abstract |
The invention discloses a quinazoline derivative containing an ethyleneimine ring side chain as shown in formula I, or their enantiomers, which mainly use 4-arylaminoquinazoline as the mother nucleus, The target compound was obtained by one-step condensation with aziridinecarboxylic acid and subsequent modification. Experiments have proved that it has a significant inhibitory effect on the proliferation of tumor cells related to EGFR tyrosine kinase activity at the cellular level (human epidermal cancer cell line A431 overexpressing EGFR, human lung adenocarcinoma cell line H1975 resistant to Gefitinib), In particular, it has a good inhibitory effect on the drug-resistant cell line H1975, and also has a good inhibitory effect on EGFR kinase, and can prepare corresponding anti-tumor cell drugs. General structural formula: . |