Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides

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 reacti...

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Detalles Bibliográficos
Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10298512/
https://www.ncbi.nlm.nih.gov/pubmed/37373075
http://dx.doi.org/10.3390/ijms24129927
Descripción
Sumario: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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