ISSN print edition: 0366-6352
ISSN electronic edition: 1336-9075
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Design, synthesis and biological study of potent and covalent HER-2 tyrosine kinase inhibitors with low cytotoxicity in vitro

Shuyu Jin, Xiuyun Sun, Dan Liu, Hua Xie, and Yu Rao

Shenyang Pharmaceutical University, Shenyang, People’s Republic of China



Abstract: The discovery and development of a novel HER-2 tyrosine kinase inhibitor for the treatment of HER2-positive breast cancer are presented in this article. EGFR family has been recognized as a crucial meditator in the cancer progression; HER-2 tyrosine kinase was one of the members among them. In the effort to explore potent HER-2 inhibitors, a novel series of 4-anilino-3-cyanoquinoline derivatives have been designed, synthesized and evaluated. Most compounds possessed modest proliferation inhibition on SK-BR-3 cell line and HER-2 kinase. Compound 16 appeared to be the most potent compound (HER-2 kinase IC50: 19.4 nM, SK-BR-3 IC50: 94 nM). In the experiment of cellular cytotoxicity assay, compound 16 shows a much lower cytotoxicity than neratinib on Beas-2b cell line (Human bronchial epithelial cells). In conclusion, compound 16 would be a promising lead compound for further anti-breast cancer drug discovery.

Keywords: HER-2 inhibitors ; 4-Anilino-3-cyanoquinoline ; Covalent ; Anticancer activity 

Full paper is available at

DOI: 10.1007/s11696-019-00686-0


Chemical Papers 73 (6) 1333–1345 (2019)

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