Synthesis and Evaluation of the Tetracyclic Ring-System of Isocryptolepine and Regioisomers for Antimalarial, Antiproliferative and Antimicrobial Activities

A series of novel quinoline-based tetracyclic ring-systems were synthesized and evaluated in vitro for their antiplasmodial, antiproliferative and antimicrobial activities. The novel hydroiodide salts <b>10</b> and <b>21</b> showed the most promising antiplasmodial inhibition...

وصف كامل

التفاصيل البيبلوغرافية
الحاوية / القاعدة:Molecules
المؤلفون الرئيسيون: Katja S. Håheim, Emil Lindbäck, Kah Ni Tan, Marte Albrigtsen, Ida T. Urdal Helgeland, Clémence Lauga, Théodora Matringe, Emily K. Kennedy, Jeanette H. Andersen, Vicky M. Avery, Magne O. Sydnes
التنسيق: مقال
اللغة:الإنجليزية
منشور في: MDPI AG 2021-05-01
الموضوعات:
الوصول للمادة أونلاين:https://www.mdpi.com/1420-3049/26/11/3268
الوصف
الملخص:A series of novel quinoline-based tetracyclic ring-systems were synthesized and evaluated in vitro for their antiplasmodial, antiproliferative and antimicrobial activities. The novel hydroiodide salts <b>10</b> and <b>21</b> showed the most promising antiplasmodial inhibition, with compound <b>10</b> displaying higher selectivity than the employed standards. The antiproliferative assay revealed novel pyridophenanthridine <b>4b</b> to be significantly more active against human prostate cancer (IC<sub>50</sub> = 24 nM) than Puromycin (IC<sub>50</sub> = 270 nM) and Doxorubicin (IC<sub>50</sub> = 830 nM), which are used for clinical treatment. Pyridocarbazoles <b>9</b> was also moderately effective against all the employed cancer cell lines and moreover showed excellent biofilm inhibition (<b>9a</b>: MBIC = 100 µM; <b>9b</b>: MBIC = 100 µM).
تدمد:1420-3049