Recent Developments of Small Molecule EGFR Inhibitors Based on the Quinazoline Core Scaffolds

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Recent Developments of Small Molecule EGFR Inhibitors Based on the Quinazoline Core Scaffolds

Anti-Cancer Agents in Medicinal Chemistry, 12(4): 391-406.

Author(s): Yu-Jing Liu, Cheng-Mei Zhang and Zhao-Peng Liu.

Affiliation: Department of Organic Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, P. R. China.


Progress in identifying and understanding the molecular and cellular causes of cancer has led to the discovery of anomalies that characterize cancer cells and that represent targets for the development of cancer therapeutics. One such target is the epidermal growth factor receptor (EGFR), a transmembrane protein that is frequently dysregulated in cancer cells and associated with the development, progression and aggressiveness of a number of malignancies. Inhibition of EGFR signaling has thus been identified as an attractive strategy in control of tumor proliferation, and over a decade of intense activity in the field has culminated in the discoveries and subsequent approvals of gefitinib and erlotinib for the treatment of non-small cell lung cancer. However, the drug's resistance to gefitinib and erlotinib has been clinically observed. Therefore, intensive efforts have been made in the discovery of novel potent and selective EGFR inhibitors. This review will focus on the developments of small molecule EGFR inhibitors based on the quinazoline core scaffolds in recent 5 years. Diverse EGFR inhibitors are classified as 4-anilinoquinazolines and 4-nonanilininoquinazolines, their biological data are described, and the structure-activity relationships (SARs) are discussed.


Anilinoquinazolines, Anti-tumor, ATP-binding, Cytotoxicity, Dual inhibitors, EGFR, HER2, ligands, Irreversible EGFR inhibitors, Nonanilininoquinazolines, EGFR inhibitors, Reversible EGFR inhibitors, SAR .

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Article Details

Volume: 12
Issue Number: 4
First Page: 391
Last Page: 406
Page Count: 16
DOI: 10.2174/187152012800228652
Price: $58
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