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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.

  作者 Causey, Patrick W.;Besanger, Travis R.;Valliant, John F.;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-9;  页码  2833-2844  
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[摘要](Organometallic and Organometalloidal Compounds) Section A series of mono- and diaryl-substituted rhenium(I) closo-2,1,8-rhenacarboranes were prepd. by microwave-assisted reaction of closo-carborane with [Re(CO)3(H2O)3]Br and screened for their affinity for two isoforms of the estrogen receptor (ER). The 2,1,8-rhenadicarbadodecaboranes [1-R1-8-R-2,1,8-Re(CO)3C2B9H9]- (1d R = 4-HOC6H4, R1 = H; 1e R = 1,4-C6H4OCH2CH2NMe2, R1 = H; 2d R = 4-HOC6H4, R1 = Ph; 2e R = 1,4-C6H4OCH2CH2NMe2, R1 = Ph; 3d R = R1 = 4-HOC6H4; 3e R = R1 = 1,4-C6H4OCH2CH2NMe2), were prepd. by boron-for-rhenium cage substitution in the corresponding 1-R-2-R1-1,2-C2B10H10 with [Re(CO)3(H2O)3]Br followed by a recently discovered spontaneous cage isomerization process, and the neutral nitrosylated analog [1-R1-8-R-2,1,8-Re(CO)2(NO)] (R = 4-HOC6H4, R1 = H) showed the highest affinities of the compds. screened. As a result, and specific activity in a manner that is suitable for routine prodn. in support of future preclin. and mol. imaging studies.

 
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