Add time:08/31/2019         Source:sciencedirect.com

IntroductionSeveral lines of evidence suggest that 7α-substituted estradiol derivatives bind to the estrogen receptor (ER). In line with this hypothesis, we designed and synthesized 18F-labeled 7α-fluoroalkylestradiol (Cn-7α-[18F]FES) derivatives as molecular probes for visualizing ERs. Previously, we successfully synthesized 7α-(3-[18F]fluoropropyl)estradiol (C3-7α-[18F]FES) and showed promising results for quantification of ER density in vivo, although extensive metabolism was observed in rodents. Therefore, optimization of the alkyl side chain length is needed to obtain suitable radioligands based on Cn-7α-substituted estradiol pharmacophores.

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