Хроман-4-онові каркаси як платформа для пошуку протиракових та противірусних сполук-лідерів

• Datum: 2025
• Hauptverfasser: Timokhin, Oleksii S., Moskvina, Viktoriia S., Kucher, Olexandr V., Keith, Kathy A., Harden, Emma A., Hartline, Caroll B., James, Scott H., Brovarets, Volodymyr S.
• Format: Artikel
• Sprache: English
• Veröffentlicht: V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine 2025
• Schlagworte: оксигеновмісні гетероцикли; хроман-4-они; антипроліферативна активність; протиракова активність; противірусна активність
• Online Zugang: https://bioorganica.com.ua/index.php/journal/article/view/96
• Назва журналу: Ukrainica Bioorganica Acta

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 such as 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 biologically active agents and identify compound 6 as a preliminary lead for further investigation of its antiviral potential