Structure-Activity Relationship Studies Based on Quinazoline Derivatives as EGFR Kinase Inhibitors (2017-Present).
4-anilino-quinazoline
EGFR
allosteric inhibitor
competitive inhibitor
covalent inhibitor
quinazoline
structure–activity relationship
Journal
Pharmaceuticals (Basel, Switzerland)
ISSN: 1424-8247
Titre abrégé: Pharmaceuticals (Basel)
Pays: Switzerland
ID NLM: 101238453
Informations de publication
Date de publication:
03 Apr 2023
03 Apr 2023
Historique:
received:
09
03
2023
revised:
28
03
2023
accepted:
31
03
2023
medline:
28
4
2023
pubmed:
28
4
2023
entrez:
28
4
2023
Statut:
epublish
Résumé
The epidermal growth factor receptor (EGFR) plays a critical role in the tumorigenesis of various forms of cancer. Targeting the mutant forms of EGFR has been identified as an attractive therapeutic approach and led to the approval of three generations of inhibitors. The quinazoline core has emerged as a favorable scaffold for the development of novel EGFR inhibitors due to increased affinity for the active site of EGFR kinase. Currently, there are five first-generation (gefitinib, erlotinib, lapatinib, vandetanib, and icotinib) and two second-generation (afatinib and dacomitinib) quinazoline-based EGFR inhibitors approved for the treatment of various types of cancers. The aim of this review is to outline the structural modulations favorable for the inhibitory activity toward both common mutant (del19 and L858R) and resistance-conferring mutant (T790M and C797S) EGFR forms, and provide an overview of the newly synthesized quinazoline derivatives as potentially competitive, covalent or allosteric inhibitors of EGFR.
Identifiants
pubmed: 37111291
pii: ph16040534
doi: 10.3390/ph16040534
pmc: PMC10141396
pii:
doi:
Types de publication
Journal Article
Review
Langues
eng
Subventions
Organisme : Iuliu Hatieganu" University of Medicine and Pharmacy, Cluj-Napoca, Romania
ID : PCD 881/45/12.01.2022
Organisme : "Iuliu Hatieganu" University of Medicine and Pharmacy, Cluj-Napoca, Romania
ID : PCD 772/36/11.01.2023
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