新型基于2,2-二甲基-2,3-二氢喹啉-4(1H)-酮的查耳酮作为细胞毒性剂的设计、合成与评价
Design, synthesis and evaluation of novel 2,2-dimethyl-2,3-dihydroquinolin-4(1H)-one based chalcones as cytotoxic agents.
作者信息
Jean Julie, Farrell David S, Farrelly Angela M, Toomey Sinead, Barlow James W
机构信息
Department of Chemistry, RCSI, 123 Stephen's Green, Dublin 2, Ireland.
Department of Medical Oncology, RCSI Education & Research Centre, Beaumont Hospital, Beaumont, Dublin 9, Ireland.
出版信息
Heliyon. 2018 Sep 4;4(9):e00767. doi: 10.1016/j.heliyon.2018.e00767. eCollection 2018 Sep.
We designed and synthesised a series of novel chalcones, incorporating the heterocyclic framework of 2,2-dimethyl-2,3-dihydro-4(1H)-quinolinone, which was prepared via Sonogashira coupling of a substituted orthoaniline under aqueous conditions using Pd catalysis followed by acid-mediated cyclisation. The compounds were screened against the NCI-N87 and DLD-1 cancer cell lines, with most compounds showing low micromolar cytotoxic activity.
我们设计并合成了一系列新型查尔酮，其包含2,2 - 二甲基 - 2,3 - 二氢 - 4(1H)-喹啉酮的杂环骨架，该骨架是通过在水相条件下使用钯催化使取代邻苯胺进行Sonogashira偶联反应，随后经酸介导环化反应制备而成。这些化合物针对NCI - N87和DLD - 1癌细胞系进行了筛选，大多数化合物显示出低微摩尔浓度的细胞毒性活性。
Zotero 插件