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合成含钆米非司酮缀合物及其在人乳腺癌细胞中孕激素受体亲和力的体外研究和结合位点的评估。

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

机构信息

Department of Chemistry-Biology, University of Quebec at Trois-Rivieres, 3351-boul. Des Forges, Trois-Rivieres, Quebec, Canada.

出版信息

Bioorg Med Chem. 2010 Mar 1;18(5):1891-8. doi: 10.1016/j.bmc.2010.01.048. Epub 2010 Jan 25.

Abstract

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.

摘要

新型基于钆的米非司酮缀合物通过各种合成路线合成。通过碱性磷酸酶(AP)测定法在人乳腺癌细胞(T47-D 细胞)中观察到新缀合物具有中等的抗孕激素活性。通过电感耦合等离子体质谱法(ICPMS)测定的结合的 Gd 量表明每个细胞的结合位点数。这些缀合物可能是开发受体靶向 MRI 对比剂以及其他抗乳腺癌治疗剂的重要化合物。

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