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

Alexandru Șandor; Ioana Ionuț; Gabriel Marc; Ilioara Oniga; Dan Eniu; Ovidiu Oniga

doi:10.3390/ph16040534

journal article Open Access Apr 03, 2023

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

Alexandru Șandor

Ioana Ionuț Gabriel Marc

Ilioara Oniga

Dan Eniu Ovidiu Oniga

Pharmaceuticals Vol. 16 No. 4 pp. 534 · MDPI AG

View at Publisher Save 10.3390/ph16040534

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.

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Details

Published: Apr 03, 2023
Vol/Issue: 16(4)
Pages: 534
License: View

Authors

A

Alexandru Șandor

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

I

Ioana Ionuț

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

G

Gabriel Marc

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

I

Ilioara Oniga

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

D

Dan Eniu

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

O

Ovidiu Oniga

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

Funding

“Iuliu Hatieganu” University of Medicine and Pharmacy, Cluj-Napoca, Romania Award: PCD 881/45/12.01.2022

Cite This Article

Alexandru Șandor, Ioana Ionuț, Gabriel Marc, et al. (2023). Structure–Activity Relationship Studies Based on Quinazoline Derivatives as EGFR Kinase Inhibitors (2017–Present). Pharmaceuticals, 16(4), 534. https://doi.org/10.3390/ph16040534

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

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