98256-65-6Relevant academic research and scientific papers
A facile and improved synthesis of 17α-{2-(E)-[125I]-iodovinyl}-19-nortestosterone, a no-carrier-added ligand for progesterone receptor analyses
Damodaran,Epperly,Pillai,Bloomer
, p. 17 - 26 (1994)
Strategies for human breast cancer therapy using 125I-labeled steroid hormones are clinically attractive in light of the estrogen dependence of and progestogen receptor involvement in many cancers and the favorable microdosimetry resulting from 125I decay. We have synthesized the no-carrier-added progesterone receptor ligand 17α-{2-(E)-[125I]-iodovinyl}-19-nortestosterone (E-125IVNNT) by a simple and high yielding method, and determined its uptake and specific progesterone receptor binding in vitro using T47D human breast carcinoma cells. The ligand was prepared by [125I]-iododestannylation of 17α-[2-(E)-tri-n-butylstannylvinyl]-19-nortestosterone (E-TBSVNNT) by using the rare iodinating agent [125I]-sodium iodide/ferric sulfate in mixed dichloromethane-water solvent. Cell binding assays demonstrated that E-125IVNNT binding to T47D breast carcinoma was specific and saturable with an affinity for the progesterone receptor 10-fold greater than that of 3H-R5020.
