Chemical synthesis of fluorinated and iodinated 17β-HSD3 inhibitors and evaluation for imaging prostate cancer tumors and tissue biodistribution

Bioorganic Chemistry(2022)

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摘要
•17β-Hydroxysteroid dehydrogenase type 3 inhibitor 1 accumulates in prostate tumor.•Fluorinated and iodinated analogs of 17β-HSD3 inhibitor 1 were efficiently synthesized.•18F-radiolabelled analog of 1 was synthesized for PET imaging/biodistribution studies.•Given orally in mice, para-iodo analog of 1 was the most metabolically stable inhibitor.
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关键词
Imaging,Hydroxysteroid dehydrogenase,17β-HSD3,Enzyme inhibitor,Steroid,Chemical synthesis,Prostate cancer,Molecular modeling
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