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RUDN University chemists have proposed a new reaction for the synthesis of complex organic substances in a single vessel

RUDN University chemists have proposed a new reaction for the synthesis of complex organic substances in a single vessel

Russian chemists have proposed a new reaction for the synthesis of complex organic substances in a single vessel. The resulting products were effective against cancer cells, including those resistant to known drugs.

The synthesis of many organic substances is a complex multi-stage process, at each stage of which only one of the necessary chemical bonds is usually formed. The desired molecule is assembled gradually, like a constructor. It takes much less time to synthesize the domino reaction — a cascade of reactions that occur together in one vessel one after another without additional reagents. Chemists from RUDN University, together with Italian colleagues, picked up substances that trigger a domino reaction to produce derivatives of chromenoisoquinolinamines. These compounds are used as anti-inflammatory and antitumor drugs, and some of them are promising candidates for the treatment of Alzheimer’s disease.

Scientists have proposed using salicylic aldehyde (a derivative of salicylic acid) and homophthalonitrile, and as a catalyst for the reaction — a cheap and environmentally friendly ammonium salt of formic acid. The initial reagents were mixed with water and isopropyl alcohol and irradiated in a microwave reactor, heated to 150 °C for 20 minutes. By reacting aldehydes with different substituent groups, the researchers obtained 19 different derivatives of chromenoisoquinolinamines.

The chemists then tested their effects on breast cancer cells, colon cancer cells, and three ovarian cancer cell lines. For comparison, cisplatin, a drug used in chemotherapy, was used. Two ovarian cancer cell lines were resistant to cisplatin, but the new substances were toxic to all tumor cells. The researchers selected two compounds that were effective even at low concentrations. Computer simulations have shown that this is due to an additional amino group that forms stable bonds with nucleotides in the DNA of the cancer cell.

“Our work was aimed at finding new compounds with promising properties for medical chemistry and creating ways to synthesize them. The developed approach makes it possible to synthesize substances with antitumor potential in one domino reaction, which proceeds very efficiently — four new chemical bonds are created in one synthetic operation. In the future, we plan to develop the created methodology by developing three — and four-component reactions based on it,” said co-author of the article Alexey Festa.

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Biologists from RUDN University discovered the secret of flaxseed oil with long shelf life

Biologists from RUDN University working together with their colleagues from the Institute of Molecular Biology of the Russian Academy of Sciences and the Institute of Flax studied the genes that determine the fatty acid composition in flaxseed oil and identified polymorphisms in six of them. The team also found out what gene variations could extend the shelf life of flaxseed oil. This data can be used to improve the genetic selection of new flax breeds. The results were published in the BMC Plant Biology journal.

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11 Oct
Mowing Is More Harmful to Soil Than Grazing

A team of biologists analyzed soil samples from a pasture and a regularly mowed meadow and found out that grazing lets more carbon get into the soil than mowing. This, in turn, improves the carbon cycle and makes microorganisms more efficient.

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11 Oct
Soil scientists suggest method for remediating urban garden soils contaminated with lead and arsenic

The soils of urban gardens and vegetable patches contain a lot of toxicants (including lead and arsenic) in high concentrations which can be harmful to the health of children and people with chronic diseases. A team of soil scientists from RUDN University suggested a remediation method developed based on data collected in a garden of Brooklyn (NY, U.S.).

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