Synthesis, in vitro progesterone receptors affinity of gadolinium containing mifepristone conjugates and estimation of binding sites in human breast cancer cells

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• 作者：Pijus Saha ; Claudia Hö ; dl ; Wolfgang S.L. Strauss ; Rudolf Steiner ; Walter Goessler ; Olaf Kunert ; Alex ; er Leitner ; Ernst Haslinger ; H. Wolfgang Schramm
• 关键词：Gadolinium-based mifepristone conjugates ; Antiprogestagenic activity ; Proton relaxation ; Progesterone binding sites ; T47-D human breast cancer cells
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2010
• 出版时间：1 March 2010
• 年：2010
• 卷：18
• 期：5
• 页码：1891-1898
• 全文大小：297 K

文摘

Novel gadolinium-based mifepristone conjugates were synthesised using various synthetic routes. Moderate antiprogestagenic activity of the new conjugates was observed in human breast cancer cells (T47-D cells) using AP (alkaline phosphatase) assay. The amount of incorporated Gd determined by inductively coupled plasma mass spectroscopy (ICPMS) indicates the number of binding sites per cell. These conjugates might be important compounds to develop receptor-targeted MRI contrast agents as well as other anti-breast cancer therapeutics.