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Updated: Sep 19, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
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The current status of quinazoline hybrids with antibreast cancer therapeutic potential-part II
Huanhong Zeng1, Minxue Zhuang1, Feili Cai1
1Department of Breast Surgery, Shengli Clinical Medical College of Fujian Medical University, Fujian Provincial Hospital, Fuzhou University Affiliated Provincial Hospital, Fuzhou, China.
Abstract:
Breast cancer, characterized by the unchecked proliferation of breast cells, which usually leads to invasive behaviors and metastatic spread, is a pervasive and multifaceted disease and remains the foremost cause of death in women across the world. Tens of chemotherapeutics have already been approved for breast cancer therapy, but multidrug resistance and severe side effects have increased both mortality and morbidity as a consequence of treatment failures, creating an urgent need to develop novel chemotherapeutics. Quinazoline hybrids with structural variations could affect breast cancer in distinct manners and have the potential to enhance efficacy, reduce side effects, and address multidrug resistance. Moreover, several quinazoline hybrids, which are exemplified by tucatinib and lapatinib, have already been applied in clinics for the treatment of breast cancer, revealing that quinazoline hybrids are valuable entities for the exploitation of novel antibreast cancer chemotherapeutics. This review outlines the current status of quinazoline hybrids with antibreast cancer potential, covering articles published from 2020 onwards. The structure-activity relationships (SARs) and mechanisms of action are also discussed to provide a potential avenue for developing more effective antibreast cancer candidates.
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