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Homodimeric and heterodimeric bis(amino thiol) oxometal complexes with rhenium(V) and technetium(V). Control of heterodimeric complex formation and an approach to metal complexes that mimic steroid hormones

Journal Article · · Journal of Medicinal Chemistry
; ;  [1]; ;  [2]
  1. Univ. of Illinois, Urbana, IL (United States). Dept. of Chemistry
  2. Washington Univ. Medical School, St. Louis, MO (United States). Mallinckrodt Institute of Radiology

The authors have investigated the possibility of preparing complexes of rhenium and technetium whose shape resembles that of ligands for steroid receptors. The general structure of N{sub 2}S{sub 2} complexes of oxorhenium (V) and oxotechnetium(V) is such that they could replace the BC ring system of steroid, thereby generating a metal complex system with considerable size and shape similarity to a steroid. Such a metal-integrated steroid-shaped complex can be constructed as a heterodimer of two different amino thiols, complexes of rhenium and technetium with such heterodimeric bis-bidentate structure have not been systematically studied. In this investigation, they have shown that complexes of this nature form readily when appropriate metal precursors are combined with a mixture of amino thiols. In the systems the authors have studied, heterodimeric complex formation is preferred over homodimeric complex formation, and in one system where they were able to obtain an x-ray crystal structure, this oxorhenium heterodimer had the desired trans geometry. These rhenium and technetium-99m complexes are reasonably stable toward ligand exchange; they can be readily purified by chromatography under appropriate conditions, and the one technetium-99m complex studied in vivo shows some persistence in blood and gives good initial uptake in several complex studied in vivo shows some persistence in blood and gives good initial uptake in several tissues. The convenient and selective formation of such bis-bidentate heterodimeric complexes suggests that the development of metal-integrated complexes that resemble ligands for receptors may be possible.

Sponsoring Organization:
USDOE
DOE Contract Number:
FG02-84ER60218
OSTI ID:
136710
Journal Information:
Journal of Medicinal Chemistry, Journal Name: Journal of Medicinal Chemistry Journal Issue: 7 Vol. 37; ISSN JMCMAR; ISSN 0022-2623
Country of Publication:
United States
Language:
English