Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Quinoxaline Derivatives in Cancer Therapy: Insights into Mechanisms of Action and Therapeutic Applications

  • Jinan Alhuwayshil (College of Pharmacy King Saud Bin Abdulaziz University for Health Sciences) ;
  • Nouf Alnajim (College of Pharmacy King Saud Bin Abdulaziz University for Health Sciences) ;
  • Sarah bin Dulaym (College of Pharmacy King Saud Bin Abdulaziz University for Health Sciences) ;
  • Jehan Alamre (Department of Clinical Pharmacology, Faculty of Medicine, King Abdul-Aziz University) ;
  • Arwa Alsubait (Medical Research Core Facility and Platforms Department, King Abdullah International Medical Research Center (KAIMRC), Ministry of National Guard Health Affairs) ;
  • Afrah E Mohammed (Department of Biology, College of Science, Princess Nourah bint Abdulrahman University) ;
  • Sahar S. Alghamdi (College of Pharmacy King Saud Bin Abdulaziz University for Health Sciences)
  • Received : 2025.03.26
  • Accepted : 2026.01.28
  • Published : 2026.03.01
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Abstract

Cancer continues to be a leading cause of morbidity and mortality globally, which necessitates the development of more effective and less toxic therapies. Quinoxaline derivatives, a class of heterocyclic compounds with versatile chemical structures, have emerged as promising candidates for anticancer drug development. These derivatives exhibit a range of biological activities and have shown significant efficacy against various tumors. However, the therapeutic potential of quinoxaline derivatives, particularly in clinical applications, remains underexplored, highlighting the need for further research to optimize their use as anticancer agents. This systematic review aims to provide an updated analysis of quinoxaline derivatives' anticancer potential, focusing on their mechanisms of action and therapeutic applications in oncology. Following PRISMA guidelines, a thorough search was conducted in MEDLINE/PubMed and Science Direct for studies from 2020 to 2024. Relevant keywords were used to identify studies on quinoxaline derivatives and their anticancer properties, resulting in the selection of 77 studies based on pharmacological activity and mechanisms. The review included 77 studies exploring various anticancer activities of quinoxaline derivatives. Key findings indicate that these compounds effectively inhibit cancer cell growth through multiple mechanisms, including the inhibition of topoisomerases, kinases, and other critical proteins involved in cancer progression. Additionally, they demonstrate strong anti-proliferative and pro-apoptotic effects across several cancer cell lines, highlighting their broad therapeutic potential. Quinoxaline derivatives represent a promising class of compounds in anticancer therapy due to their diverse biological activities and multiple molecular targets. The development of these derivatives as targeted therapies holds the potential for more effective cancer treatments.

Keywords

Acknowledgement

The authors sincerely thank the College of Pharmacy at King Saud bin Abdulaziz University for Health Sciences (KSAU-HS) for their ongoing support. We also express our profound gratitude to the Department of Pharmacology and Histology at King Abdul-Aziz University for their invaluable contributions, which greatly aided in the completion of this paper. This research was funded by King Abdullah International Medical Research Center (KAIMRC), the Ministry of National Guard Health Affairs, Riyadh, and the Kingdom of Saudi Arabia under the grant agreement number (SPR24/006/5).

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