一种新型苯胺基-3H-吡咯并[3,2-f]喹啉衍生物作为潜在抗癌剂的发现。
Discovery of a new anilino-3H-pyrrolo[3,2-f]quinoline derivative as potential anti-cancer agent.
作者信息
Via L Dalla, Gia O, Gasparotto V, Ferlin M G
机构信息
Department of Pharmaceutical Sciences, University of Padova, Via Marzolo 5, 35131 Padova, Italy.
出版信息
Eur J Med Chem. 2008 Feb;43(2):429-34. doi: 10.1016/j.ejmech.2007.04.008. Epub 2007 May 6.
The newly synthesized 1-[4-(3H-pyrrolo[3,2-f]quinolin-9-ylamino)-phenyl]-ethanone hydrochloride showed high antiproliferative activity by mixed mechanisms of action. The compound acts by forming an intercalative complex with DNA and inhibiting DNA topoisomerase II (topo II) and by blocking the cell cycle in G(2)/M phase. Probable cell death by apoptosis is also suggested by flow cytometry analysis.
新合成的盐酸1-[4-(3H-吡咯并[3,2-f]喹啉-9-基氨基)-苯基]-乙酮通过混合作用机制显示出高抗增殖活性。该化合物通过与DNA形成嵌入复合物、抑制DNA拓扑异构酶II（拓扑II）以及在G(2)/M期阻断细胞周期发挥作用。流式细胞术分析也提示可能通过凋亡导致细胞死亡。
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