2-Phenylbenzothiazole conjugated with cyclopentadienyl tricarbonyl [CpM(CO)3] (M = Re, (99m)Tc) complexes as potential imaging probes for β-amyloid plaques

Dalton Transactions : an International Journal of Inorganic Chemistry
Jianhua JiaBoli Liu

Abstract

Technetium-99m-labeled cyclopentadienyl tricarbonyl complexes conjugated with the 2-phenylbenzothiazole binding motif were synthesized. The rhenium surrogates , , and were demonstrated to have moderate to high affinities for Aβ1-42 aggregates with Ki values of 142, 76, 64 and 24 nM, respectively. During the fluorescence staining of brain sections of transgenic mice and patients with Alzheimer's disease, these rhenium complexes demonstrated perfect and intense labeling of Aβ plaques. Moreover, in in vitro autoradiography, (99m)Tc-labeled complexes clearly detected β-amyloid plaques on sections of brain tissue from transgenic mice, which confirmed the sufficient affinity of these tracers for Aβ plaques. However, these compounds did not show desirable properties in vivo, especially showing poor brain uptake (below 0.5% ID g(-1)), which will hinder the further development of these tracers as brain imaging agents. Nonetheless, it is encouraging that these (99m)Tc-labeled complexes designed by a conjugate approach displayed sufficient affinities for Aβ plaques.

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Citations

May 18, 2016·Scientific Reports·Shimpei IikuniHideo Saji
Jul 28, 2016·Inorganic Chemistry·David J HaynePaul S Donnelly
Sep 19, 2016·European Journal of Medicinal Chemistry·Jianhua JiaMengchao Cui
Jun 8, 2018·Dalton Transactions : an International Journal of Inorganic Chemistry·Jinhui WangSuzanne Fery-Forgues
Apr 12, 2018·Current Medicinal Chemistry·Sajjad MolavipordanjaniSeyed Jalal Hosseinimehr
Oct 22, 2019·Future Medicinal Chemistry·Arantxa Pino-CuevasEzequiel M Vázquez-López
Feb 6, 2018·Future Medicinal Chemistry·Hao LiuXiaohui Wang
Mar 10, 2017·MedChemComm·S ChaturvediAnil K Mishra
Apr 23, 2020·Frontiers in Chemistry·Stephan MokeschBernhard K Keppler
Oct 24, 2017·ACS Medicinal Chemistry Letters·Christos KiritsisMaria Pelecanou
Nov 9, 2021·Dalton Transactions : an International Journal of Inorganic Chemistry·Dumisani V KamaAndreas Roodt
Nov 25, 2021·Chemical Communications : Chem Comm·Raphael LengacherRoger Alberto

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