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Updated: Sep 13, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
The current landscape of quinazoline derivatives with in vivo anticancer therapeutic potential-part II
Shanshan Huang1, Zhi Xu1, Yan Zhang2
1School of Chemistry and Pharmaceutical Engineering, Huanghuai University, Zhumadian, Henan, China.
Abstract:
Cancer, which can invade and metastasize to almost all organs or tissues, is one of the deadliest diseases across the world. Drug resistance, especially multidrug resistance, is a principal obstacle to effective therapeutic interventions against cancer, creating an urgent demand for the exploration of novel anticancer chemotherapeutics. Quinazoline derivatives are useful templates for exploring new anticancer chemotherapeutics due to their ability to exert anticancer effects through various mechanisms, mainly associated with alterations in cell cycle progression, induction of apoptosis, and modification of autophagy. Moreover, tens of quinazoline-based agents have already been approved for cancer therapy, occupying a prominent place in the current therapeutic arsenal. This review provides an overview of the current status of quinazoline derivatives that hold in vivo anticancer therapeutic potential, along with their mechanisms of action, toxicity profiles, and pharmacokinetic characteristics, encompassing literature published from 2015 to the present.
Insights
Quinazoline derivatives show promise as novel anticancer drugs, offering new therapeutic strategies to overcome drug resistance in cancer treatment. This review highlights their potential and mechanisms of action.
Area of Science:
- Medicinal Chemistry
- Oncology
- Pharmacology
Background:
- Cancer remains a leading global cause of death, with drug resistance posing a significant challenge.
- Multidrug resistance in cancer necessitates the development of novel chemotherapeutic agents.
- Quinazoline derivatives are recognized for their diverse anticancer activities and established therapeutic roles.
Purpose of the Study:
- To review the in vivo anticancer potential of quinazoline derivatives.
- To explore the mechanisms of action, toxicity, and pharmacokinetics of these compounds.
- To provide an updated overview of recent advancements in quinazoline-based cancer therapeutics.
Main Methods:
- Comprehensive literature search for studies published from 2015 to the present.
- Analysis of research focusing on quinazoline derivatives with demonstrated in vivo anticancer activity.
- Evaluation of reported mechanisms, toxicity profiles, and pharmacokinetic data.
Main Results:
- Quinazoline derivatives exhibit anticancer effects via cell cycle arrest, apoptosis induction, and autophagy modulation.
- Several quinazoline-based agents have shown significant in vivo efficacy in preclinical models.
- The review details the therapeutic potential, safety, and drug-like properties of various derivatives.
Conclusions:
- Quinazoline derivatives represent a valuable class of compounds for developing next-generation anticancer therapies.
- Understanding their mechanisms and properties is crucial for advancing their clinical application.
- Continued research into quinazoline derivatives holds significant promise for overcoming cancer drug resistance.
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