异卡波肼四环系统及其区域异构物的合成与评价及抗疟、抗增殖和抗微生物活性。
Synthesis and Evaluation of the Tetracyclic Ring-System of Isocryptolepine and Regioiso-Mers for Antimalarial, Antiproliferative and Antimicrobial Activities.
机构信息
Department of Chemistry, Bioscience and Environmental Engineering, University of Stavanger, NO-4036 Stavanger, Norway.
Discovery Biology, Griffith Institute for Drug Discovery, Griffith University, Don Young Road, Nathan, QLD 4111, Australia.
出版信息
Molecules. 2021 May 30;26(11):3268. doi: 10.3390/molecules26113268.
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 and showed the most promising antiplasmodial inhibition, with compound displaying higher selectivity than the employed standards. The antiproliferative assay revealed novel pyridophenanthridine to be significantly more active against human prostate cancer (IC = 24 nM) than Puromycin (IC = 270 nM) and Doxorubicin (IC = 830 nM), which are used for clinical treatment. Pyridocarbazoles was also moderately effective against all the employed cancer cell lines and moreover showed excellent biofilm inhibition (: MBIC = 100 µM; : MBIC = 100 µM).
一系列新型基于喹啉的四环环系被合成并在体外评估其抗疟原虫、抗增殖和抗微生物活性。新型氢碘酸盐盐 和 显示出最有前途的抗疟原虫抑制作用，化合物 比所使用的标准品具有更高的选择性。增殖测定显示新型吡啶并菲啶 对人前列腺癌（IC = 24 nM）的活性明显高于用于临床治疗的 Puromycin（IC = 270 nM）和 Doxorubicin（IC = 830 nM）。吡啶并咔唑 对所有使用的癌细胞系也具有中等活性，此外对生物膜抑制具有优异的作用（：MBIC = 100 µM；：MBIC = 100 µM）。
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