Synthesis and screening of mono- and di-aryl technetium and rhenium metallocarboranes. A new class of probes for the estrogen receptor.
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 2B9H9)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'C2B9H9)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.
Causey
Patrick W
PW
The McMaster Nuclear Reactor, McMaster University, Hamilton, Ontario L8S 4M1, Canada.
Besanger
Travis R
TR
Valliant
John F
JF
D001896:Boron Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D018360:Crystallography, X-Ray; D047628:Estrogen Receptor alpha / Q000737:chemistry*; D047629:Estrogen Receptor beta / Q000737:chemistry*; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D015609:Organotechnetium Compounds / Q000138:chemical synthesis / Q000737:chemistry; D020033:Protein Isoforms / Q000378:metabolism; D011869:Radioligand Assay; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D012211:Rhenium; D013329:Structure-Activity Relationship; D013667:Technetium
D001896:Boron Compounds; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D008024:Ligands; D009942:Organometallic Compounds; D015609:Organotechnetium Compounds; D020033:Protein Isoforms; D019275:Radiopharmaceuticals; D012211:Rhenium; D013667:Technetium