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18 February 2022 11:33

Small molecules for “big” drugs

People need new drugs: antiviral, antimicrobial, antitumor. As a rule, they are developed by large pharmaceutical corporations that have great budgets and unlimited opportunities. However, small academic groups are also trying to find active substances for new drugs. Due to the breakthrough results of these groups, their countries can be competitive in the global pharmaceutical market.

One of such groups also works at Danylo Halytsky Lviv National Medical University. Scientists are implementing the project “Thiazolidinones with polypharmacological properties: molecular design, synthesis and mechanisms of action of anti-cancer, anti-inflammatory and antimicrobial agents”. This project won the call «Support for Research of Leading and Young Scientists» and received grant funding in the amount of 12 million UAH.

The project supervisor is the Head of the Department of Pharmaceutical, Organic and Bioorganic Chemistry of the LNMU Roman Lesyk. Together with his team they decided to investigate properties of heterocyclic thiazolidinone derivatives to synthesize new active molecules.

– It turns out that small molecules we synthesize can have several properties at the same time – Roman explained. – One molecule can be active against microbes, viruses, oncocells, etc., ie have antitumor, anti-inflammatory, antimicrobial, antiviral, anti-TB properties.

The scientist is convinced that these new molecules can become prototypes of drugs. Moreover, he has an ambitious goal not only to synthesize such a molecule, but also to work on creating new drugs in the future.

A large group of new molecules has been obtained already, new methods for the synthesis of heterocyclic compounds have been developed, in particular, about a hundred molecules with antitumor activity have been obtained (tested in vitro on cancer cells). Some of them are already being studied in vivo by animals.

Molecules with high antimicrobial activity have also been identified.

– We’ve found that these molecules work on antibiotic-resistant strains of microorganisms, – explains Roman. – This is extremely important, because antibiotic resistance is a problem of global importance. Today, doctors are sounding the alarm and warning that the effectiveness of modern antibiotics is declining. This means that in the fight against disease humanity risks being discarded to decades ago…

By the way, scientists have found that synthesized molecules have a trypanosomal effect (trypanosomes are parasites that cause sleeping sickness). According to the scientist, sleeping sickness, unfortunately, is not interesting for the “big farm”, because it affects mainly in Africa. Since 1990, no drug has been developed for this disease (and these molecules are active against leishmaniasis, another parasite that is not easy to destroy).

As part of the project, researchers are collaborating with colleagues from 21 countries. Many universities around the world have already learned about the research of Ukrainian scientists, they write letters to scientists and are interested in their successes. – We send letters to each other, we involve experts – Roman smiles. – It helps a lot at work.

Scientists also cooperate with Ukrainian colleagues, in particular, with specialists from the Institute of Cell Biology of the National Academy of Sciences of Ukraine. The team, led by Roman, consists of seven researchers. Six (!) of them are young scientists.

– It is very important to unite smart people in a team, to give the opportunity to be successful, to be realized in the academic space – the researcher emphasizes. – It is impossible to do without good equipment. With the help of the NRFU grant funding we bought an elemental analyzer, devices for biological research (we have never had such before). It is the first time when we have all the necessary reagents. I see how this experience is changing the psychology of young people. Young scientists work on modern equipment and receive a decent salary. They understand that they can be competitive in the world of science. It is very important.

We asked the project supervisor – What advice would you give to your colleagues who plan to participate in the future NRFU calls? What does victory require?

– We need an honest selection of scientists for the team, – he answers without the slightest hesitation. – it is necessary to involve in project those who really work. Even a famous name is not enough! I am convinced that in these three years new names should appear in research teams, new people, who have achieved breakthrough successes in the implementation of projects.

The scientist is also convinced that there is no need to be afraid of defeat. Times when reviews were copied are gone and applications are meticulously analyzed now, so there is no big deal in a negative response. It is important not to stop, use this experience, write a perfect application and win.

Svitlana GALATA

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