Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides
Trifonov A.V. Gazizov A.S. Tapalova A.S. Kibardina L.K. Appazov N.O. Voloshina A.D. Sapunova A.S. Luybina A.P. Abyzbekova G.M. Dobrynin A.B. Litvinov I.A. Tauekel A.K. Yespenbetova S.O. Burilov A.R. Pudovik M.A.
June 2023Multidisciplinary Digital Publishing Institute (MDPI)
International Journal of Molecular Sciences
2023#24Issue 12
Herein, we report the design and synthesis of novel 7-aza-coumarine-3-carboxamides via scaffold-hopping strategy and evaluation of their in vitro anticancer activity. Additionally, the improved non-catalytic synthesis of 7-azacoumarin-3-carboxylic acid is reported, which features water as the reaction medium and provides a convenient alternative to the known methods. The anticancer activity of the most potent 7-aza-coumarine-3-carboxamides against the HuTu 80 cell line is equal to that of reference Doxorubicin, while the selectivity towards the normal cell line is 9–14 fold higher.
amides , anti-tumor , aza-coumarine , cytotoxicity , selectivity
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Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Science, Arbuzova Str., 8, Kazan, 420088, Russian Federation
Korkyt Ata Kyzylorda University, Aiteke Bi Street, 29A, Kyzylorda, 120014, Kazakhstan
Department of Oil, Chemistry and Nanotechnology, Kazan National Research Technological University, Karl Marx Str., 68, Kazan, 420015, Russian Federation
Arbuzov Institute of Organic and Physical Chemistry
Korkyt Ata Kyzylorda University
Department of Oil
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