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Synthesis, in vitro progesterone receptors affinity of gadolinium containing mifepristone conjugates and estimation of binding sites in human breast cancer cells.
Saha, Pijus; Hödl, Claudia; Strauss, Wolfgang S L; Steiner, Rudolf; Goessler, Walter; Kunert, Olaf; Leitner, Alexander; Haslinger, Ernst; Schramm, H Wolfgang.
Afiliação
  • Saha P; Department of Chemistry-Biology, University of Quebec at Trois-Rivieres, 3351-boul. Des Forges, Trois-Rivieres, Quebec, Canada. pijus.saha@uqtr.ca
Bioorg Med Chem ; 18(5): 1891-8, 2010 Mar 01.
Article em En | MEDLINE | ID: mdl-20149664
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.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Mama / Receptores de Progesterona / Mifepristona / Complexos de Coordenação / Gadolínio Limite: Female / Humans Idioma: En Ano de publicação: 2010 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Mama / Receptores de Progesterona / Mifepristona / Complexos de Coordenação / Gadolínio Limite: Female / Humans Idioma: En Ano de publicação: 2010 Tipo de documento: Article