AUTHOR=Ma Zhaowu , Woon Clariis Yi-Ning , Liu Chen-Guang , Cheng Jun-Ting , You Mingliang , Sethi Gautam , Wong Andrea Li-Ann , Ho Paul Chi-Lui , Zhang Daping , Ong Peishi , Wang Lingzhi , Goh Boon-Cher TITLE=Repurposing Artemisinin and its Derivatives as Anticancer Drugs: A Chance or Challenge? JOURNAL=Frontiers in Pharmacology VOLUME=Volume 12 - 2021 YEAR=2021 URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2021.828856 DOI=10.3389/fphar.2021.828856 ISSN=1663-9812 ABSTRACT=

Cancer has become a global health problem, accounting for one out of six deaths. Despite the recent advances in cancer therapy, there is still an ever-growing need for readily accessible new therapies. The process of drug discovery and development is arduous and takes many years, and while it is ongoing, the time for the current lead compounds to reach clinical trial phase is very long. Drug repurposing has recently gained significant attention as it expedites the process of discovering new entities for anticancer therapy. One such potential candidate is the antimalarial drug, artemisinin that has shown anticancer activities in vitro and in vivo. In this review, major molecular and cellular mechanisms underlying the anticancer effect of artemisinin and its derivatives are summarised. Furthermore, major mechanisms of action and some key signaling pathways of this group of compounds have been reviewed to explore potential targets that contribute to the proliferation and metastasis of tumor cells. Despite its established profile in malaria treatment, pharmacokinetic properties, anticancer potency, and current formulations that hinder the clinical translation of artemisinin as an anticancer agent, have been discussed. Finally, potential solutions or new strategies are identified to overcome the bottlenecks in repurposing artemisinin-type compounds as anticancer drugs.