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

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.
Pijus Saha 1,  Claudia Hödl,  Wolfgang S L Strauss,  Rudolf Steiner,  Walter Goessler,  Olaf Kunert,  Alexander Leitner,  Ernst Haslinger,  H Wolfgang Schramm
Affiliations

Affiliation

  • 1 Department of Chemistry-Biology, University of Quebec at Trois-Rivieres, 3351-boul. Des Forges, Trois-Rivieres, Quebec, Canada. [email protected]
PMID: 20149664 DOI: 10.1016/j.bmc.2010.01.048
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.

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