Abstract
4-Anilinoquinazoline derivatives possess high anti-cancer activities. Many of them are highly selective tyrosine kinase inhibitors (TKI), particularly against epidermal growth factor receptor (EGFR). EGFRs are overexpressed or mutated in most carcinomas and are required for tumor progression. The efficacy of EGFR-targeted anti-tumor drugs is impaired by drug-induced acquired resistance. Therefore, there is urgency to find better anti-cancer agents with novel effects on EGFR. 4-Anilinoquinazolines are small molecule EGFR inhibitors that have been synthesized and assessed for their anti-tumor bioactivity. In this paper, we review the 4-anilinoquinazoline derivatives with EGFR inhibitor activity reported in recent years.
Keywords: 4-anilinoquinazoline, Anti-tumor activity, Epidermal growth factor receptor (EGFR).
Graphical Abstract
Anti-Cancer Agents in Medicinal Chemistry
Title:4-Anilinoquinazoline Derivatives with Epidermal Growth Factor Receptor Inhibitor Activity
Volume: 16 Issue: 12
Author(s): Fang Liu, Baoding Tang, Hao Liu, Leina Li, Gang Liu, Yun Cheng, Yan Xu, Wenwen Chen and Yinjiu Huang
Affiliation:
Keywords: 4-anilinoquinazoline, Anti-tumor activity, Epidermal growth factor receptor (EGFR).
Abstract: 4-Anilinoquinazoline derivatives possess high anti-cancer activities. Many of them are highly selective tyrosine kinase inhibitors (TKI), particularly against epidermal growth factor receptor (EGFR). EGFRs are overexpressed or mutated in most carcinomas and are required for tumor progression. The efficacy of EGFR-targeted anti-tumor drugs is impaired by drug-induced acquired resistance. Therefore, there is urgency to find better anti-cancer agents with novel effects on EGFR. 4-Anilinoquinazolines are small molecule EGFR inhibitors that have been synthesized and assessed for their anti-tumor bioactivity. In this paper, we review the 4-anilinoquinazoline derivatives with EGFR inhibitor activity reported in recent years.
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Cite this article as:
Liu Fang, Tang Baoding, Liu Hao, Li Leina, Liu Gang, Cheng Yun, Xu Yan, Chen Wenwen and Huang Yinjiu, 4-Anilinoquinazoline Derivatives with Epidermal Growth Factor Receptor Inhibitor Activity, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (12) . https://dx.doi.org/10.2174/1871520616666160404113141
DOI https://dx.doi.org/10.2174/1871520616666160404113141 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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