4
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.

Visiting Professors View all
03 Nov 2017
Michele Pagano is a graduate of the University of Pisa, a leading scientist, the author of more than 200 publications in international journals, and a participant in many international research projects
1885
Main Publications View all
15 Nov 2017
RUDN University scientists publish results of their scientific researches in highly-recognized in whole world and indexed in international databases journals (Web of Science, Scopus ect.). That, of course, corresponds to the high status of the University and its international recognition. Publications of June-September 2017 ( In Journals of categories Q1-Q3)
1203
Similar newsletter View all
31 Mar
RUDN University awards for specific areas of science and technology based on the results of 2021

Every year, RUDN University selects the best of the best in the field of science and innovation and encourages with a special reward. Since 2009, the Academic Council of the University has been awarding one reward in natural and technical sciences and the other one in social and humanitarian sciences. Both individual researchers and groups of authors can become laureates.

66
31 Mar
International Day of Women and Girls in Science: women scientists of the RUDN talk about their path to science

“Science is the basis of all progress that facilitates the life of mankind and reduces its suffering,” — Marie Sklodowska—Curie. A symbol of a woman’s success in science. The first scientist in the world — twice winner of the Nobel Prize.

308
31 Mar
RUDN University Mathematicians Create a Model for Queue Organizing with Self-Sustained Servers

RUDN University mathematicians proposed a model for optimizing the operation of queuing systems (from computer networks to stores). Unlike analogues, the servers in it are self-sustained. They can determine when to start and stop working themselves. Such a model can be useful, for example, for online taxi services and other systems where workers choose their own operating hours.

75
Similar newsletter View all