Cancer patients often face more than the disease itself. Their treatment is frequently complicated by infections and other health conditions, meaning they may need to take several different medications at once. As the number of prescribed drugs increases, so does the risk of interactions between them, which is why scientists are searching for solutions that could one day address multiple problems with a single compound.
In collaboration with partners, researchers at Kaunas University of Technology (KTU) have developed new hybrid compounds that, in laboratory studies, were shown to simultaneously reduce the viability of aggressive cancer cells and inhibit the growth of certain bacteria and fungi.
Study Tested Lung Cancer, Breast Cancer and Melanoma Cells
“A hybrid molecule is a dual-action compound that combines two or more active structures capable of acting on different biological targets. Such hybrid molecules can affect several biological mechanisms at the same time, which may increase treatment effectiveness and reduce the likelihood of cells developing resistance,” explains Aida Šermukšnytė, a PhD student at the KTU Department of Organic Chemistry.
According to Dr Ingrida Tumosienė, a researcher at the Department of Organic Chemistry, the development of such compounds is driven by two major challenges in modern medicine – aggressive forms of cancer and the growing antimicrobial resistance. The researcher says this is precisely why the development of such compounds is currently regarded as one of the most promising directions in drug development.
The potential of the newly developed compounds was evaluated using cells from some of the most aggressive forms of cancer – lung cancer, triple-negative breast cancer and melanoma. As Dr Kristina Kantminienė, Associate Professor at the KTU Department of Physical and Inorganic Chemistry and Senior Researcher on the project at the Department of Organic Chemistry, explains, these tumours were selected because they carry a high risk of metastasis, are often resistant to existing drugs, and treatment options remain limited. This makes the search for new treatments for these cancers particularly important.
Laboratory studies showed that some of the compounds reduced cancer cell viability – in other words, the affected cells either died or stopped multiplying. However, as Kantminienė emphasises, this does not mean that a cure for cancer has been discovered.
“This study provides only an initial indication that the compound warrants further investigation,” she says.
Compound Outperformed Currently Used Drugs
The antimicrobial results were equally noteworthy. Three of the synthesised compounds showed strong activity against bacteria and fungi. One proved more effective against fungi than nystatin, the antifungal drug used as a control, while its antibacterial activity was comparable to that of the antibiotic vancomycin. Two other compounds also produced very promising results, with their activity in some cases matching or even exceeding the effectiveness of currently used medicines.
The researchers were surprised to find that the compound showing the strongest dual action – both anticancer and antimicrobial – was not the one they had expected to perform best. According to the scientists, this once again demonstrated that every stage of research is important when developing new drug candidates, from theoretical calculations to laboratory experiments.
“We know what effects we are looking for and which structural fragments are likely to give new molecules these properties,” says Tumosienė. She explains that the entire process is cyclical: based on the results obtained, the molecules are continuously refined until the most promising compounds are identified.
Although there is still a long way to go before any potential drug could be developed, the researchers regard these results as an important step forward. The next stages will require a more detailed investigation of the mechanisms of action of the most promising compounds and their effects on healthy cells, followed by preclinical and clinical studies and further optimisation of the molecules themselves. Only then will it be possible to determine whether the compounds developed in the laboratory today could eventually serve as the basis for new medicinal substances.
The study was carried out as part of the project PYRANCAM (Agreement No. S-MIP-25-22), funded by the Research Council of Lithuania under the Researcher Groups funding scheme. According to the KTU researchers, the results presented in the article build on previous research and contribute to international efforts in medicinal chemistry to find new solutions both for treating cancer and combating antimicrobial resistance.
The scientific article “New hybrid pyridine–1,2,4-triazole scaffolds: synthesis, in vitro evaluation of anticancer and antimicrobial activity, and in silico insights” can be found here.