Synthesis of novel gefitinib-based derivatives and their anticancer activity.

Drug latentiation is a process of modifying a drug molecule structurally to improve its binding affinity as well as increasing the drug-receptor interactions and potentiate its therapeutic potential. In the quest for discovering more potent epidermal growth factor receptor (EGFR) inhibitors, gefitinib-based derivatives were designed by simple structural modification at the secondary amine of gefitinib by N-alkylation. Three gefitinib derivatives (gefitinib-NB, -NP, and -NIP) were synthesized by N-alkylation and phase transfer catalysis.