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Synthesis and Screening of Mono- and Di-Aryl Technetium and Rhenium Metallocarboranes. A New Class of Probes for the Estrogen Receptor.

Causey PW, Besanger TR, Valliant JF

The McMaster Nuclear Reactor, McMaster University, Hamilton, Ontario L8S 4M1, Canada, Departments of Chemistry and Medical Physics & Applied Radiation Sciences, McMaster University, 1280 Main Street West, Hamilton, Ontario L8S 4M1, Canada valliant@mcmaster.ca.

A series of mono and diaryl rhenium(I)-carborane derivatives were prepared using microwave heating and screened for their affinity for two isoforms of the estrogen receptor (ER). The rhenacarborane derivative [(RR'C 2B 9H 9)Re(CO) 3] (-) (R = p-PhOH, R' = H), which was generated by taking advantage of a recently discovered cage isomerization process, and the neutral nitrosated analogue [(RR'C 2B 9H 9)Re(CO) 2(NO)] (R = p-PhOH, R' = H) showed the highest affinities of the compounds screened. As a result, the (99m)Tc analogue of one of the leads was produced in high yield (84%) and specific activity in a manner that is suitable for routine production in support of future preclinical and molecular imaging studies.

Published 5 May 2008 in J Med Chem, 51(9): 2833-2844.
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