Synthesis, in vitro progesterone receptors affinity of gadolinium containing mifepristone conjugates and estimation of binding sites in human breast cancer cells.
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.
Saha
Pijus
P
Department of Chemistry-Biology, University of Quebec at Trois-Rivieres, 3351-boul. Des Forges, Trois-Rivieres, Quebec, Canada. pijus.saha@uqtr.ca
Hödl
Claudia
C
Strauss
Wolfgang S L
WS
Steiner
Rudolf
R
Goessler
Walter
W
Kunert
Olaf
O
Leitner
Alexander
A
Haslinger
Ernst
E
Schramm
H Wolfgang
HW
D001665:Binding Sites; D001943:Breast Neoplasms / Q000175:diagnosis* / Q000188:drug therapy; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry; D005260:Female; D005682:Gadolinium / Q000737:chemistry*; D006801:Humans; D008279:Magnetic Resonance Imaging; D015735:Mifepristone / Q000138:chemical synthesis / Q000737:chemistry*; D011980:Receptors, Progesterone / Q000037:antagonists & inhibitors / Q000378:metabolism*
D056831:Coordination Complexes; D011980:Receptors, Progesterone; D015735:Mifepristone; D005682:Gadolinium