title: Epidermal growth factor receptor inhibitors: a patent review (2010 - present).
abstract: BACKGROUND
  The signaling pathways downstream of epidermal growth factor receptor (EGFR) are central to the biology of colorectal cancer. EGFR kinase represents an attractive target for the development of novel therapies for the treatment of cancers. A considerable achievement during the past 2 years was the development of targeted therapies against EGFR using small-molecule inhibitors such as quinazoline derivatives, pyrimidine derivatives, thiazole derivatives, acrylamide derivatives and urea derivatives. Some new methods and technologies were also used to discover novel reversible and irreversible EGFR inhibitors. In this review, recent advances in the research of EGFR inhibitors are reviewed.
  
  
  METHODS
  This review summarized new patents and articles published on EGFR inhibitors within 2010 to present.
  
  
  CONCLUSIONS
  From 2010 to present, some novel scaffolds have been discovered as first-generation EGFR inhibitors, which are more potent against both EGFR-activating (EGFR WT) and resistance mutations (EGFRDM, T790M/L858R). 'Fast-Forwarding Hit to Lead' and 'Combi-Molecule' postulate to represent a novel approach to cancer therapy. The focus on irreversible inhibitors is also of significance for the design of kinase inhibitors. Searching nature for novel scaffolds is a promising way to find new chemical tools with which we can better understand the development of drug resistance to current targeted therapy and study ways to bypass and overcome such drug resistance.
authors.affiliation: Soochow University, College of Pharmaceutical Science , Suzhou 215123 , PR China.
authors.forename: Si-Ning
authors.initials: SN
authors.lastname: Li
authors.forename: Huan-Qiu
authors.initials: HQ
authors.lastname: Li
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000627:therapeutic use*; D015195:Drug Design; D019008:Drug Resistance, Neoplasm; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D006801:Humans; D007880:Legislation, Drug; D015394:Molecular Structure; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000235:genetics / Q000473:pathology; D010330:Patents as Topic; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D066246:ErbB Receptors