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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 anticancer therapeutic potential, along with their mechanisms of action, toxicity profiles, and pharmacokinetic characteristics, encompassing literature published from 2015 to the present.
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http://dx.doi.org/10.1080/17568919.2025.2539670 | DOI Listing |
J Med Chem
September 2025
Key Laboratory of Marine Drugs and Key Laboratory of Evolution and Marine Biodiversity (Ministry of Education), School of Medicine and Pharmacy, Institute of Evolution & Marine Biodiversity, Ocean University of China, Qingdao 266003, China.
BRD4, a bromodomain-containing protein, has emerged as an attractive therapeutic target for various diseases. Selective inhibition of the bromodomain is gaining traction as a promising strategy for targeted drug discovery. Based on bioisosterism-guided optimization of RVX-OH (), a pan-BET inhibitor, we designed and synthesized a series of novel quinazolin-4(3)-one derivatives as potent BRD4 inhibitors.
View Article and Find Full Text PDFACS Chem Neurosci
September 2025
Department of Pharmaceutical Chemistry, L. M. College of Pharmacy, Ahmedabad, Gujarat 380009, India.
The Keap1-Nrf2 pathway has emerged as a promising target for Alzheimer's disease (AD). This study employed modeling to identify Nrf2 activators through Keap1 inhibition. The most promising quinazoline derivative, LMDP10, was then evaluated in a rat model of sporadic AD induced by Intracerebroventricular (ICV) streptozotocin (STZ).
View Article and Find Full Text PDFRSC Adv
August 2025
Pharmaceutical Medicinal Chemistry& Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University Cairo 11884 Egypt
A novel series of quinazoline-based compounds were designed and synthesized as modified analogues to certain known VEGFR-2 inhibitors, as an extension of our work on the design and synthesis of new VEGFR-2 inhibitors. The anti-proliferative properties of the synthesized compounds were assessed against three tumor cell lines (MCF-7, HepG-2, and K-562). Compounds 8a (IC = 0.
View Article and Find Full Text PDFBMJ Open
August 2025
Department of Endocrinology, Endocrine and Metabolic Disease Medical Center, Nanjing Drum Tower Hospital, Affiliated Hospital of Medical School, Nanjing University, Nanjing, Jiangsu, China
Introduction: Diabetes is a significant modifiable risk factor for cognitive dysfunction. There are currently no effective treatments that delay or reverse the progression of cognitive dysfunction. Accumulating evidence demonstrates that specific antidiabetes medications hold promise in improving cognitive function.
View Article and Find Full Text PDFJ Med Chem
August 2025
State Key Laboratory of Anti-Infective Drug Discovery and Development, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, P. R. China.
This work describes the discovery of a new series of Aurora kinase inhibitors based on quinazoline skeleton derived from , as well as the first X-ray cocrystal structure complexes of vinyl-quinazoline with Aurora A. Replacing pyrimidine with quinazoline improved anticancer activity and facilitated cocrystal formation. Compounds and showed excellent Aurora A kinase inhibition, with IC values of 6.
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