Synthesis and Evaluation of the Tetracyclic Ring-System of Isocryptolepine and Regioisomers for Antimalarial, Antiproliferative and Antimicrobial Activities
作者: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
DOI:10.3390/molecules26113268
日期:——
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 10 and 21 showed the most promising antiplasmodial inhibition, with compound 10 displaying higher selectivity than the employed standards. The antiproliferative assay revealed novel pyridophenanthridine
合成了一系列新的基于喹啉的四环系统,并在体外评估了它们的抗疟原虫、抗增殖和抗菌活性。新型氢碘酸盐10和21显示出最有希望的抗疟原虫抑制作用,化合物10显示出比所用标准更高的选择性。抗增殖试验显示新型吡啶并菲啶4b对人前列腺癌 (IC 50 = 24 nM) 的活性明显高于用于临床治疗的嘌呤霉素 (IC 50 = 270 nM) 和多柔比星 (IC 50 = 830 nM)。吡啶并咔唑9对所有采用的癌细胞系也具有中等效果,此外还显示出出色的生物膜抑制(9a:MBIC = 100 µM;9b:MBIC = 100 µM)。