奥昔芬净衍生物的合成与抗增殖评估
Syntheses and antiproliferative evaluation of oxyphenisatin derivatives.
作者信息
Uddin Muhammed K, Reignier Serge G, Coulter Tom, Montalbetti Christian, Grånäs Charlotta, Butcher Steven, Krog-Jensen Christian, Felding Jakob
机构信息
Evotec(UK) Ltd, 111 Milton Park, Abingdon, Oxon OX14 4RX, UK.
出版信息
Bioorg Med Chem Lett. 2007 May 15;17(10):2854-7. doi: 10.1016/j.bmcl.2007.02.060. Epub 2007 Feb 25.
Syntheses and structure-antiproliferative relationship for oxyphenisatin analogues are described. The cell proliferation data showed that the presence of substituents (especially F, Cl, Me, CF(3), and OMe) in the 6- and 7-position of oxyphenisatin markedly enhanced the potency in the MDA-468 cell line without affecting the MDA-231 cell line. The best compounds from this series showed low nanomolar antiproliferative activity towards the MDA-468 cell line and a 1000-fold selectivity over the MDA-231 cell line.
本文描述了氧化菲尼辛类似物的合成及其结构与抗增殖活性的关系。细胞增殖数据表明，在氧化菲尼辛的6位和7位引入取代基（尤其是F、Cl、Me、CF(3)和OMe）可显著增强其对MDA - 468细胞系的活性，而对MDA - 231细胞系无影响。该系列中最佳的化合物对MDA - 468细胞系显示出低纳摩尔级的抗增殖活性，且对MDA - 231细胞系具有1000倍的选择性。
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