Scientists from ITMO and the Arbuzov Institute of Organic and Physical Chemistry have synthesized chemical compounds that can selectively destroy cancer cells without affecting healthy ones. This was reported to RT by the press service of ITMO. The study was supported by the Russian Science Foundation. The results are published in the journal Bioorganic Chemistry.

As the authors remind, most of the drugs used today for cancer chemotherapy have significant drawbacks: high toxicity and low selectivity. Such drugs not only affect tumor cells, but also negatively affect healthy ones, which leads to consequences such as weakened immune system, hair loss, loss of appetite, damage to the mucous membrane of the mouth and throat, etc.

Experts have proposed a new, point method for the treatment of cancerous tumors. To do this, they synthesized nine chemical compounds based on macromolecules, products of the synthesis of phenol and formaldehyde - calixarenes. Chemists have attached pyrazole fragments to these molecular platforms - they are able to bind to the DNA molecule.

  • Anton Muravyov
  • © ITMO. NEWS / Dmitry Grigoriev

Next, the scientists in the laboratory treated the resulting compounds with six cell lines: four cancerous and two healthy. As a result, three compounds suppressed the activity of cervical carcinoma cells, and healthy cells, including chemotherapy-sensitive liver cells, retained their viability.

"We were inspired by this result, because it indicates low toxicity. Further, we were convinced in experiments with blood that red blood cells are not destroyed in the presence of calixarenes, "said Anton Muravyov.

Experiments on mice have also shown that, compared with classical chemotherapy drugs, the toxicity of new compounds is almost ten times lower for normal cells. At the same time, the effect on cancer cells is the opposite: in cervical carcinoma, when interacting with compounds, apoptosis was triggered - programmed cell death.

"This was achieved largely due to the correctly selected geometry of compounds with "replaced" pyrazole fragments. In addition, we identified a target molecule in the cells that binds to our drug - it turned out to be DNA, "explains Anton Muravyov.

Now the authors of the study intend to test the resulting compounds for mutagenicity - the ability to cause genetic mutations in cells, as well as to find out exactly how they interact with the DNA of cancer cells at the molecular level. In the future, the obtained compounds may become the basis for promising anti-cancer drugs of selective action.