Syntheses and antiproliferative evaluation of oxyphenisatin derivatives

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• 作者：Muhammed K. Uddin ; Serge G. Reignier ; Tom Coulter ; Christian Montalbetti ; Charlotta Grå ; nä ; s ; Steven Butcher ; Christian Krog-Jensen ; Jakob Felding
• 关键词：Antiproliferative ; Anticancer ; MDA-468 cell line ; Phenisatin ; Whole cell assay
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 出版时间：15 May 2007
• 年：2007
• 卷：17
• 期：10
• 页码：2854-2857
• 全文大小：149 K

文摘

Syntheses and structure–antiproliferative relationship for oxyphenisatin analogues are described. The cell proliferation data showed that the presence of substituents (especially F, Cl, Me, CF₃, 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.