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Trifonov, Alexey V; Gazizov, Almir S; Tapalova, Anipa S; Kibardina, Lyudmila K; Appazov, Nurbol O; Voloshina, Alexandra D; Sapunova, Anastasiia S; Luybina, Anna P; Abyzbekova, Gulmira M; Dobrynin, Alexey B; Litvinov, Igor A; Tauekel, Akerke K; Yespenbetova, Sholpan O; Burilov, Alexander R; Pudovik, Michail A
International journal of molecular sciences, 06/2023, Volume: 24, Issue: 12Journal Article
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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