Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides.
Alexey V TrifonovAlmir S GazizovAnipa S TapalovaLyudmila K KibardinaNurbol Orynbasaruly AppazovAlexandra D VoloshinaAnastasiia S SapunovaAnna P LuybinaGulmira M AbyzbekovaAlexey B DobryninIgor A LitvinovAkerke K TauekelSholpan O YespenbetovaAlexander R BurilovMichail A PudovikPublished in: International journal of molecular sciences (2023)
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.
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