Design, synthesis and characterization of functionalized 1,2,4-trioxanes/trioxepanes for antimalarial and anticancer applications

The document titled “World Malaria Report-2022” indicates that malaria is still taking its toll. Approximately 619,000 people lost their lives due to this serious disease in 2021. It is worth adding that in 2021, 247 million cases of malaria were reported worldwide. Malaria, the life-threatening and most lethal infection in humans, is caused mainly by the parasite Plasmodium falciparum. The isolation of an innovative substance, artemisinin, with an endoperoxide group in its structure from the traditional Chinese herb Artemisia annua in the 1970s, became a milestone for medicine. This discovery helped save over 200 million lives over the next four decades. Currently, to reduce the global burden of disease and slow the emergence of drug resistance, the World Health Organization (WHO) has recommended artemisinin-based combination therapy as a “first-line drug” for the treatment of malaria. Like malaria, cancer represents another significant threat to human life, accounting for almost 10 million deaths annually (2020 data). In addition to promising antimalarial activity, several artemisinin-based endoperoxides have also shown promising anticancer activity in various clinical trials. Unfortunately, drug-resistant and multidrug-resistant (MDR) Plasmodium strains appear as a result of mutations in numerous drug transporter genes. A similar problem also affects cancer treatment. Due to the lack of reliable drugs, the demand for new ones is growing. Furthermore, the anticancer activity of the most active molecules will be assessed in vivo using the chick embryo chorioallantoic membrane (CAM) model. This research will certainly bring a lot of new knowledge to antimalarial and anticancer chemotherapy, contributing to the improvement of the well-being of human societies.

Project details

Drug-based Strategies
Product Development

Nov 2023 — Nov 2026

$232,493

Poland