Diastereoselective Synthesis of Novel Spiro-Phosphacoumarins and Evaluation of Their Anti-Cancer Activity
Sennikova V.V. Zalaltdinova A.V. Sadykova Y.M. Khamatgalimov A.R. Gazizov A.S. Voloshina A.D. Lyubina A.P. Amerhanova S.K. Voronina J.K. Chugunova E.A. Appazov N.O. Burilov A.R. Pudovik M.A.
November 2022MDPI
International Journal of Molecular Sciences
2022#23Issue 22
Herein we present the regio- and diastereoselective synthesis of novel pyrrolidine-fused spiro-dihydrophosphacoumarins via intermolecular [3 + 2] cycloaddition reaction. The presented approach is complementary to existing ones and provides an easy entry to the otherwise inaccessible derivatives. Additionally, the unprecedented pathway of the reaction of 4-hydroxycoumarin with azomethine ylides is described. The anti-cancer activity of the obtained compounds was tested in vitro, the most potent compound being 2.6-fold more active against the HuTu 80 cell line than the reference 5-fluorouracil, with a selectivity index > 32.
anti-cancer , azomethine ylide , cycloaddition , cytotoxicity , phosphacoumarin , quantum chemistry
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Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Arbuzova str. 8, Kazan, 420088, Russian Federation
Institute of General and Inorganic Chemistry, Russian Academy of Sciences, Leninsky Ave. 31, Moscow, 119991, Russian Federation
Korkyt Ata Kyzylorda State University, 29A Aiteke Bi St., Kyzylorda, 120014, Kazakhstan
Arbuzov Institute of Organic and Physical Chemistry
Institute of General and Inorganic Chemistry
Korkyt Ata Kyzylorda State University
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