Bio-Evaluation of ^99mTc-Labeled Homodimeric Chalcone Derivative as Amyloid-β-Targeting Probe.

ABSTRACT: Chalcone derivatives have been successfully utilized for a range of biological applications and can cross the blood-brain barrier easily. β-amyloid-specific bis-chalcone derivative, 6,9-bis(carboxymethyl)-14-(4-[(E)-3-(4-(dimethylamino)phenyl)acryloyl]phenoxy)-3-(2-[(2-(4-[(E)-3-(4-(dimethylamino)phenyl)acryloyl]phenoxy)ethyl)amino]-2-oxoethyl)-11-oxo-3,6,9,12-tetraazatetradecanoic acid, DT(Ch)₂, was analyzed using molecular modeling to explain the binding modes of the ligand with amyloid fibril and monomer followed by ^99mTc-complexation in 95% yield and 98.7% efficiency. High-binding specificity of the radiocomplex was established following in vitro evaluation against 100-fold excess of DT(Ch)₂. ^99mTc-DT(Ch)₂ exhibited <3% tran

SUBMITTER: Mann G 

PROVIDER: S-EPMC9249127 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature