13α-雌酮衍生物作为潜在抗增殖剂的合成与生物学评价
Synthesis and biological evaluation of 13α-estrone derivatives as potential antiproliferative agents.
作者信息
Szabó Johanna, Pataki Zoltán, Wölfling János, Schneider Gyula, Bózsity Noémi, Minorics Renáta, Zupkó István, Mernyák Erzsébet
机构信息
Department of Organic Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, Hungary.
Department of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
出版信息
Steroids. 2016 Sep;113:14-21. doi: 10.1016/j.steroids.2016.05.010. Epub 2016 Jun 2.
13α-Estrone derivatives containing various substituents on C-3 and C-17 were synthesized, and evaluated by means of MTT assays for in vitro antiproliferative activity against a panel of human adherent cancer cell lines (HeLa, MCF-7, A2780 and A431). Compounds with N-benzyltriazolylmethoxy moieties on C-3 proved to be more potent than their 3-hydroxy or 3-ether counterparts. Some triazoles exerted substantial cytostatic effects against particular tumor cell lines, with submicromolar IC50 values.
合成了在C-3和C-17上含有各种取代基的13α-雌酮衍生物，并通过MTT法评估了它们对一组人贴壁癌细胞系（HeLa、MCF-7、A2780和A431）的体外抗增殖活性。结果表明，在C-3上带有N-苄基三唑基甲氧基部分的化合物比其3-羟基或3-醚类似物更具活性。一些三唑对特定肿瘤细胞系具有显著的细胞生长抑制作用，IC50值在亚微摩尔范围内。
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