Current Medicinal Chemistry

Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge


Insight into the Medicinal Chemistry of EGFR and HER-2 Inhibitors

Author(s): C. Wang, H. Gao, J. Dong, F. Wang, P. Li and J. Zhang

Affiliation: School of Medicine, Xi'an Jiaotong University, No. 76, Yanta West Road, 710061, Xi'an, ShaanXi Province, P.R. China.


Dysregulation of receptor tyrosine kinases (RTKs) in cancer cells is extremely common. Overexpression of human epidermal growth factor receptor (EGFR/HER) tyrosine kinase is correlated with tumor aetiology, progression and poor prognosis. Their activation is also observed frequently in human cancers. Therefore, RTKs have been identified as important therapeutic targets in oncology. Many therapeutic methods have been developed based on inhibition of EGFR and HER-2. Herein, we will discuss recent progress in the development of EGFR/HER-2 tyrosine kinase inhibitors. We will focus on the design strategies, pharmacological profiles and structure-activity relationships (SARs) of EGFR and HER-2 inhibitors.

Keywords: EGFR, ERBB, HER-2, structure-activity relationship, tyrosine kinase.

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Article Details

Page: [1336 - 1350]
Pages: 15
DOI: 10.2174/0929867320666131119124646