title: Development of the Third Generation EGFR Tyrosine Kinase Inhibitors for Anticancer Therapy.
abstract: Epidermal growth factor receptor (EGFR) is one of the most important targets in anticancer therapy. Till date, a large number of first and second generation EGFR tyrosine kinase inhibitors (TKIs) have been marketed or advanced into clinical studies. However, the occurrence of TKI-resistant mutations has led to the loss of efficacy of these inhibitors. In the purpose of overcoming resistant mutations and reducing side effects, lots of third generation EGFR inhibitors are explored with promising potencies against EGFR mutations while sparing wild-type EGFR. This review outlines the current landscape of the development of third generation EGFR inhibitors, mainly focusing on the biological properties, clinical status and structure-activity relationships.
authors.affiliation: Department of Pharmacy, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China. 11019016@zju.edu.cn.
authors.forename: Weiyan
authors.initials: W
authors.lastname: Cheng
authors.forename: Jianhua
authors.initials: J
authors.lastname: Zhou
authors.forename: Xin
authors.initials: X
authors.lastname: Tian
authors.affiliation: . firstph@163.com.
authors.forename: Xiaojian
authors.initials: X
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000627:therapeutic use; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D056004:Molecular Dynamics Simulation; D009369:Neoplasms / Q000188:drug therapy; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000627:therapeutic use; D054852:Small Molecule Libraries / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D054852:Small Molecule Libraries; D066246:ErbB Receptors