Design, Synthesis and Biological Evaluation of Lapatinib Derivatives as HER1/HER2 Inhibitors
Five Lapatinib derivatives were designed by structurally modifying the side chain as well as
the aniline substituent. The ELISA assay showed that the derivatives retained or even improved the
inhibitory activity of Lapatinib against HER1/HER2. In vitro cytotoxicity assay revealed that the derivatives significantly
inhibited the proliferation of the HER1/HER2-overexpressing cancer cells. Furthermore, molecular modeling study suggested
that the derivative could effectively enter the ATP binding pocket of HER1 and interact with the corresponding
residues in a manner similar to Lapatinib.
Keywords: Antitumor, HER1/HER2 inhibition, cytotoxicity, lapatinib derivatives.
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