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Sennikova, Valeriia V; Zalaltdinova, Alena V; Sadykova, Yulia M; Khamatgalimov, Ayrat R; Gazizov, Almir S; Voloshina, Alexandra D; Lyubina, Anna P; Amerhanova, Syumbelya K; Voronina, Julia K; Chugunova, Elena A; Appazov, Nurbol O; Burilov, Alexander R; Pudovik, Michail A
International journal of molecular sciences, 11/2022, Volume: 23, Issue: 22Journal Article
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.
