A facile and improved synthesis of 17α-{2-(E)-[1 2 5 I]-iodovinyl}-19-nortestosterone, a no-carrier-added ligand for progesterone receptor analyses
✍ Scribed by Kalyani M. Damodaran; Michael W. Epperly; K. M. R. Pillai; William D. Bloomer
- Publisher
- John Wiley and Sons
- Year
- 1994
- Tongue
- French
- Weight
- 443 KB
- Volume
- 34
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
Strategies for human breast cancer therapy using ^125^I‐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 ^125^I decay. We have synthesized the no‐carrier‐added progesterone receptor ligand 17α‐{2‐(E)‐[^125^I]‐iodovinyl}‐19‐nortestosterone (E‐^125^IVNNT) 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 [^125^I]‐iododestannylation of 17α‐[2‐(E)‐tri‐n‐butylstannylvinyl]‐19‐nortestosterone (E‐TBSVNNT) by using the rare iodinating agent [^125^I]‐sodium iodide/ferric sulfate in mixed dichloromethane‐water solvent. Cell binding assays demonstrated that E‐^125^IVNNT binding to T47D breast carcinoma was specific and saturable with an affinity for the progesterone receptor 10‐fold greater than that of ^3^H‐R5020.