期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 9, 页码 2833-2844出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm701561e
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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'C2B9H9)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 Tc-99m 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.
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