Platinum-based anticancer drugs — cisplatin, oxaliplatin, and carboplatin — are used for chemotherapy in about half of cancer cases. They penetrate cells and interact with DNA molecules. The process is fatal for rapidly dividing cancer cells because the drugs prevent the duplication of DNA molecules, which is necessary for successful division. Since cancer cells divide rapidly, they are the first to be affected. Still, platinum derivatives have certain disadvantages: low stability under physiological conditions and high toxicity.
To create new drugs, a strategy that involves the development of hybrid molecules is often used in modern chemistry. Such substances consist of two or more active fragments that are linked by a linker into one molecule. They usually have a double action, characteristic of each of the fragments.
A chemist from RUDN University, candidate of biological sciences Kirill Kirsanov, created a series of new drugs: hybrids of cisplatin, lonidamine, and bexarotene. Lonidamine itself has an anti-tumour effect due to its ability to suppress energy metabolism in cancer cells. In combination with radiation therapy, it is used to treat brain tumours. Bexarotene is used for the treatment of lung cancer and breast cancer, as it inhibits the growth of tumour cells of hematopoietic and squamous origin.
A derivative of cisplatin with bexarotene turned out to be the most promising. A combination of succinic acid and ethylenediamine was used as a linker. In tests conducted on four tumour cell lines, the hybrid drug was 80 times more active than bexaroten and 20 times higher on average than cisplatin, and the new drug was 80 times more active than cisplatin on MCF7D cell line. Based on the resulting leading compound, new and more effective anti-tumour medications can be developed.
The paper was published in the journal Inorganica Chimica Acta.
Yakov Kuzyakov, a well-known soil scientist, a leading scientist at RUDN Agricultural and Technological Institute and a professor at the King Saud University, has been awarded the title of highly cited researcher in the field of agricultural sciences (according to Clarivate).
A RUDN chemist has obtained a new compound — a dumbbell-shaped phosphate-bridged molybdenum cluster. The cluster accelerates the reaction of the formation of sulfides from oxides and can be used in pharmaceutical and cosmetic manufacturing.
Mathematicians from RUDN University have studied the properties of compositional operators in spaces with mixed Lebesgue norms. It will help describe the diffusion of liquids in materials with cracks and in porous materials. Such spaces are also useful for obtaining estimates for solutions to the Navier-Stokes equation.