Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides
oleh: Alexey V. Trifonov, Almir S. Gazizov, Anipa S. Tapalova, Lyudmila K. Kibardina, Nurbol O. Appazov, Alexandra D. Voloshina, Anastasiia S. Sapunova, Anna P. Luybina, Gulmira M. Abyzbekova, Alexey B. Dobrynin, Igor A. Litvinov, Akerke K. Tauekel, Sholpan O. Yespenbetova, Alexander R. Burilov, Michail A. Pudovik
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2023-06-01 |
Deskripsi
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.