Design, Synthesis and Biological Evaluation of Lapatinib Derivatives as HER1/HER2 Inhibitors

Author(s): Aifeng Lyu, Lei Fang, Shaohua Gou, Xia Liu.

Journal Name: Letters in Drug Design & Discovery

Volume 12 , Issue 7 , 2015

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Graphical Abstract:


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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Article Details

Year: 2015
Page: [574 - 584]
Pages: 11
DOI: 10.2174/1570180812999150206111626
Price: $58

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