Structure–Activity Relationship Studies Based on Quinazoline Derivatives as EGFR Kinase Inhibitors (2017–Present)

Author:

Șandor Alexandru1ORCID,Ionuț Ioana1,Marc Gabriel1ORCID,Oniga Ilioara2ORCID,Eniu Dan3,Oniga Ovidiu1

Affiliation:

1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 41 Victor Babeș Street, 400010 Cluj-Napoca, Romania

2. Department of Pharmacognosy, “Iuliu Hatieganu” University of Medicine and Pharmacy, 12 Ion Creangă Street, 400010 Cluj-Napoca, Romania

3. Department of Surgical Oncology, “Iuliu Hațieganu” University of Medicine and Pharmacy, 34-36 Republicii Street, 40015 Cluj-Napoca, Romania

Abstract

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.

Funder

“Iuliu Hatieganu” University of Medicine and Pharmacy, Cluj-Napoca, Romania

Publisher

MDPI AG

Subject

Drug Discovery,Pharmaceutical Science,Molecular Medicine

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