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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Saha P, Hodl C, Strauss WS, Steiner R, Goessler W, Kunert O, Leitner A, Haslinger E, Schramm HW

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

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

PubMed ID

20149664 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Mifepristone	Progesterone receptor	IC 50 (nM)	0.05	N/A	N/A	Details