Discovery of Di(het)arylmethane and Dibenzoxanthene Derivatives as Potential Anticancer Agents
Smolobochkin A. Niyazova D. Gazizov A. Syzdykbayev M. Voloshina A. Amerhanova S. Lyubina A. Neganova M. Aleksandrova Y. Babaeva O. Voronina J. Appazov N. Sinyashin O. Alabugin I. Burilov A. Pudovik M.
June 2024Multidisciplinary Digital Publishing Institute (MDPI)
International Journal of Molecular Sciences
2024#25Issue 12
A family of bifunctional dihetarylmethanes and dibenzoxanthenes is assembled via a reaction of acetals containing a 2-chloroacetamide moiety with phenols and related oxygen-containing heterocycles. These compounds demonstrated selective antitumor activity associated with the induction of cell apoptosis and inhibition of the process of glycolysis. In particular, bis(heteroaryl)methane containing two 4-hydroxy-6-methyl-2H-pyran-2-one moieties combine excellent in vitro antitumor efficacy with an IC50 of 1.7 µM in HuTu-80 human duodenal adenocarcinoma models with a high selectivity index of 73. Overall, this work highlights the therapeutic potential of dimeric compounds assembled from functionalized acetals and builds a starting point for the development of a new family of anticancer agents.
anticancer agents , cytotoxic activity , di(het)arylmethane , dibenzoxanthene
Text of the article Перейти на текст статьи
Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Arbuzov Str., 8, Kazan, 420088, Russian Federation
Laboratory of Engineering Profile, Department of Engineering Technology, Korkyt Ata Kyzylorda University, Ayteke bi, Str., 29A, Kyzylorda, 120014, Kazakhstan
Nazarbayev Intellectual School Chemical-Biological Direction in Kyzylorda, Sultan Beybars Str., 6, Kyzylorda, 120014, Kazakhstan
Institute of Physiologically Active Compounds at Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Severnij pr., 1, Chernogolovka, 142432, Russian Federation
N.S. Kurnakov Institute of General and Inorganic Chemistry, Russian Academy of Sciences, Leninskii pr., 31, Moscow, 119071, Russian Federation
Limited Liability Partnership «DPS-Kyzylorda», Amangeldi Str., 112A, Kyzylorda, 120014, Kazakhstan
Department of Chemistry and Biochemistry, Florida State University, Chieftan Way Str., 95, Tallahassee, 32306-3290, FL, United States
Arbuzov Institute of Organic and Physical Chemistry
Laboratory of Engineering Profile
Nazarbayev Intellectual School Chemical-Biological Direction in Kyzylorda
Institute of Physiologically Active Compounds at Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry
N.S. Kurnakov Institute of General and Inorganic Chemistry
Limited Liability Partnership «DPS-Kyzylorda»
Department of Chemistry and Biochemistry
10 лет помогаем публиковать статьи Международный издатель
Книга Публикация научной статьи Волощук 2026 Book Publication of a scientific article 2026