作为强效抗肿瘤剂的2,3-二取代和2,2,3-三取代-3-甲氧基羰基-γ-丁内酯的合成
Synthesis of 2,3-di- and 2,2,3-trisubstituted-3-methoxycarbonyl-γ-butyrolactones as potent antitumor agents.
作者信息
Le Floch Camille, Le Gall Erwan, Sengmany Stéphane, Renevret Patrice, Léonel Eric, Martens Thierry, Cresteil Thierry
机构信息
Électrochimie et Synthèse Organique, Institut de Chimie et des Matériaux Paris-Est, UMR 7182 CNRS - Université Paris-Est Créteil, 2-8 rue Henri Dunant, 94320 Thiais, France.
Électrochimie et Synthèse Organique, Institut de Chimie et des Matériaux Paris-Est, UMR 7182 CNRS - Université Paris-Est Créteil, 2-8 rue Henri Dunant, 94320 Thiais, France.
出版信息
Eur J Med Chem. 2015 Jan 7;89:654-70. doi: 10.1016/j.ejmech.2014.10.074. Epub 2014 Oct 28.
Various 2,3-substituted γ-butyrolactones have been synthesized by three-component reaction of aryl bromides, dimethyl itaconate and carbonyl compounds. The in vitro cytotoxic activity of these products was evaluated against a representative panel of cancer cell lines (KB, HCT116, MCF7, MCF7R, PC3, SK-OV3, HL60 and HL60R). One compound (4x) displays a good anti-proliferative activity with IC50 in the sub-micromolar range. The mechanism of action has been investigated using flow cytometry.
通过芳基溴化物、衣康酸二甲酯和羰基化合物的三组分反应合成了各种2,3-取代的γ-丁内酯。针对一组具有代表性的癌细胞系（KB、HCT116、MCF7、MCF7R、PC3、SK-OV3、HL60和HL60R）评估了这些产物的体外细胞毒性活性。一种化合物（4x）表现出良好的抗增殖活性，其IC50在亚微摩尔范围内。已使用流式细胞术研究了其作用机制。
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