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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...
| Autores principales: | , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
MDPI
2023
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| Materias: | |
| 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 |
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| author | 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. |
| author_facet | 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. |
| author_sort | Trifonov, Alexey V. |
| collection | PubMed |
| description | 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. |
| format | Online Article Text |
| id | pubmed-10298512 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2023 |
| publisher | MDPI |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-102985122023-06-28 Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides 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. Int J Mol Sci 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. MDPI 2023-06-09 /pmc/articles/PMC10298512/ /pubmed/37373075 http://dx.doi.org/10.3390/ijms24129927 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
| spellingShingle | Article 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. Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides |
| title | Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides |
| title_full | Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides |
| title_fullStr | Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides |
| title_full_unstemmed | Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides |
| title_short | Synthesis and Anticancer Evaluation of Novel 7-Aza-Coumarine-3-Carboxamides |
| title_sort | synthesis and anticancer evaluation of novel 7-aza-coumarine-3-carboxamides |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10298512/ https://www.ncbi.nlm.nih.gov/pubmed/37373075 http://dx.doi.org/10.3390/ijms24129927 |
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