2,2-Дизаміщені 5- та 8-азахроман-4-они: вплив на ріст ракових клітин у порівнянні з хроманоновими аналогами
A series of 2,2-disubstituted 5-azachroman-4-ones (two examples) and isomeric 8-azachroman-4-ones (four derivatives) were evaluated for their in vitro anticancer activity on 60 cancer cell lines. The decreased proliferation of cancer cells was observed for the case of both types of isomeric azachrom...
Збережено в:
| Дата: | 2023 |
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| Автори: | , |
| Формат: | Стаття |
| Мова: | English |
| Опубліковано: |
V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine
2023
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| Теми: | |
| Онлайн доступ: | https://bioorganica.com.ua/index.php/journal/article/view/66 |
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| Назва журналу: | Ukrainica Bioorganica Acta |
Репозитарії
Ukrainica Bioorganica Acta| Резюме: | A series of 2,2-disubstituted 5-azachroman-4-ones (two examples) and isomeric 8-azachroman-4-ones (four derivatives) were evaluated for their in vitro anticancer activity on 60 cancer cell lines. The decreased proliferation of cancer cells was observed for the case of both types of isomeric azachromanones with the highest activity for 2,3,5,6-tetrahydrospiro[pyran-4,2'-pyrano[2,3-b]pyridin]-4'(3'H)-one, which slows down the growth of 27 out of 60 cancer cell lines by more than half, including melanoma, colon and ovarian cancers. The structure-activity relationship in the hit spirocyclic 8-azachromanone was established by comparison with the parent chromanone analog (the least active) and the corresponding 8-fluorosubstituted derivative (showed moderate activity) |
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