Chroman-4-one Scaffolds as a Platform for Anticancer and Antiviral Lead Discovery
Chroman-4-one derivatives, a class of oxygen-containing heterocycles commonly found in biologically active natural products, continue to attract significant attention for their potential in anticancer and antiviral drug discovery. In this study, a small library of eight chroman-4-one compounds was s...
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| Дата: | 2025 |
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| Автори: | , , , , , , , |
| Формат: | Стаття |
| Опубліковано: |
V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine
2025
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| Онлайн доступ: | https://bioorganica.com.ua/index.php/journal/article/view/96 |
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| Назва журналу: | Ukrainica Bioorganica Acta |
Репозитарії
Ukrainica Bioorganica Acta| Резюме: | Chroman-4-one derivatives, a class of oxygen-containing heterocycles commonly found in biologically active natural products, continue to attract significant attention for their potential in anticancer and antiviral drug discovery. In this study, a small library of eight chroman-4-one compounds was synthesized via Kabbe condensation and screened for antiproliferative activity against the NCI-60 human cancer cell line panel. Most compounds demonstrated low cytotoxicity at a concentration of 10 μM; however, several derivatives exhibited selective growth-inhibitory effects against specific tumor cell lines, including non-small cell lung cancer and melanoma. In parallel, 7-hydroxyspiro[chromane-2,1'-cyclohexan]-4-one (compound 6) was evaluated for antiviral activity against a panel of DNA and RNA viruses. While it showed no significant activity against RNA viruses or herpesviruses, it demonstrated selective antiviral activity against HPV-11 (EC50 = 3.35 µM, SI50 >45) and moderate activity against BK virus (EC50 = 15.88 µM, SI50 >9), with low associated cytotoxicity. These findings support the chroman-4-one scaffold as a promising chemotype for the development of selective anticancer and antiviral agents and identify compound 6 as a lead candidate for further antiviral optimization. |
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