2-(4-Hydroxyphenyl)benzothiazole dicarboxylate ester TACN chelators for 64Cu PET imaging in Alzheimer's disease

Yujue Wang; Truc T. Huynh; Nilantha Bandara; Hong Jun Cho; Buck E. Rogers; Liviu M. Mirica

doi:10.1039/d1dt02767k

2-(4-Hydroxyphenyl)benzothiazole dicarboxylate ester TACN chelators for ⁶⁴Cu PET imaging in Alzheimer's disease

Yujue Wang, Truc T. Huynh, Nilantha Bandara, Hong Jun Cho, Buck E. Rogers, Liviu M. Mirica

Research output: Contribution to journal › Article › peer-review

8 Scopus citations

Abstract

Herein we report a new series of bifunctional chelators (BFCs) with high affinity for amyloid β aggregates, strong binding affinity towards Cu(ii), and favorable lipophilicity for potential blood–brain barrier (BBB) penetration. The alkyl carboxylate ester pendant arms show high binding affinity towards Cu(ii). The BFCs form stable ⁶⁴Cu-radiolabeled complexes and exhibit favorable partition coefficient (log D) values of 0.75–0.95. Among the five compounds tested, ⁶⁴Cu-YW-1 and ⁶⁴Cu-YW-13 complexes exhibit significant staining of amyloid plaques in ex vivo autoradiography studies.

Original language	English
Pages (from-to)	1216-1224
Number of pages	9
Journal	Dalton Transactions
Volume	51
Issue number	3
DOIs	https://doi.org/10.1039/d1dt02767k
State	Published - Jan 21 2022

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title = "2-(4-Hydroxyphenyl)benzothiazole dicarboxylate ester TACN chelators for 64Cu PET imaging in Alzheimer's disease",

abstract = "Herein we report a new series of bifunctional chelators (BFCs) with high affinity for amyloid β aggregates, strong binding affinity towards Cu(ii), and favorable lipophilicity for potential blood–brain barrier (BBB) penetration. The alkyl carboxylate ester pendant arms show high binding affinity towards Cu(ii). The BFCs form stable 64Cu-radiolabeled complexes and exhibit favorable partition coefficient (log D) values of 0.75–0.95. Among the five compounds tested, 64Cu-YW-1 and 64Cu-YW-13 complexes exhibit significant staining of amyloid plaques in ex vivo autoradiography studies.",

author = "Yujue Wang and Huynh, {Truc T.} and Nilantha Bandara and Cho, {Hong Jun} and Rogers, {Buck E.} and Mirica, {Liviu M.}",

note = "Publisher Copyright: This journal is {\textcopyright} The Royal Society of Chemistry",

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month = jan,

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doi = "10.1039/d1dt02767k",

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T1 - 2-(4-Hydroxyphenyl)benzothiazole dicarboxylate ester TACN chelators for 64Cu PET imaging in Alzheimer's disease

AU - Wang, Yujue

AU - Huynh, Truc T.

AU - Bandara, Nilantha

AU - Cho, Hong Jun

AU - Rogers, Buck E.

AU - Mirica, Liviu M.

N1 - Publisher Copyright: This journal is © The Royal Society of Chemistry

PY - 2022/1/21

Y1 - 2022/1/21

N2 - Herein we report a new series of bifunctional chelators (BFCs) with high affinity for amyloid β aggregates, strong binding affinity towards Cu(ii), and favorable lipophilicity for potential blood–brain barrier (BBB) penetration. The alkyl carboxylate ester pendant arms show high binding affinity towards Cu(ii). The BFCs form stable 64Cu-radiolabeled complexes and exhibit favorable partition coefficient (log D) values of 0.75–0.95. Among the five compounds tested, 64Cu-YW-1 and 64Cu-YW-13 complexes exhibit significant staining of amyloid plaques in ex vivo autoradiography studies.

AB - Herein we report a new series of bifunctional chelators (BFCs) with high affinity for amyloid β aggregates, strong binding affinity towards Cu(ii), and favorable lipophilicity for potential blood–brain barrier (BBB) penetration. The alkyl carboxylate ester pendant arms show high binding affinity towards Cu(ii). The BFCs form stable 64Cu-radiolabeled complexes and exhibit favorable partition coefficient (log D) values of 0.75–0.95. Among the five compounds tested, 64Cu-YW-1 and 64Cu-YW-13 complexes exhibit significant staining of amyloid plaques in ex vivo autoradiography studies.

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U2 - 10.1039/d1dt02767k

DO - 10.1039/d1dt02767k

M3 - Article

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AN - SCOPUS:85123617869

SN - 1477-9226

VL - 51

SP - 1216

EP - 1224

JO - Dalton Transactions

JF - Dalton Transactions

IS - 3

ER -

2-(4-Hydroxyphenyl)benzothiazole dicarboxylate ester TACN chelators for ⁶⁴Cu PET imaging in Alzheimer's disease

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