Design and synthesis of astatinated benzothiazole compounds for their potential use in Targeted Alpha Therapy (TAT) strategies to treat Alzheimer's disease-associated amyloid plaques
Applied Radiation and Isotopes(2023)
摘要
•Iodination and astatination with boronic acid precursors.•Synthesis of an astatinated benzothiazole for the potential treatment of amyloid diseases such as Alzheimer's Disease.•Radiolabeled [211At]3′-At-PIB-OMe with 55% RCY.•[211At]3′-At-PIB-OMe showed greater than 99% radiochemical stability in 3 h in a 50:50 mixture of MeOH and PBS.
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关键词
Targeted alpha therapy,Amyloid,Radiochemistry,Astatine-211,Copper catalyzed astatination,Alzheimer's disease
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