Novel synthetic ligands for targeted PET imaging and radiotherapy of copper

Hyun Soon Chong; Santosh Mhaske; Mai Lin; Sankar Bhuniya; Hyun A. Song; Martin W. Brechbiel; Xiankai Sun

doi:10.1016/j.bmcl.2007.09.052

Novel synthetic ligands for targeted PET imaging and radiotherapy of copper

Hyun Soon Chong, Santosh Mhaske, Mai Lin, Sankar Bhuniya, Hyun A. Song, Martin W. Brechbiel, Xiankai Sun

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

28 Scopus citations

Abstract

Novel ligands, NBEA, NBPA, NETA, NE3TA, and NE3TA-Bn, were synthesized and evaluated as potential chelators of copper radioisotopes for use in targeted positron emission tomography (PET) imaging or radiation therapy. The new ligands were radiolabeled with ⁶⁴Cu, and in vitro stability of the radiolabeled complexes was assessed in rat serum. Serum stability results suggest that among the ligands tested, NETA, NE3TA, and NE3TA-Bn form stable complexes with ⁶⁴Cu.

Original language	English (US)
Pages (from-to)	6107-6110
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	22
DOIs	https://doi.org/10.1016/j.bmcl.2007.09.052
State	Published - Nov 15 2007

Keywords

Cu-64
Macrocyclic ligands
PET imaging
Serum stability
Synthetic chelates
Targeted radiotherapy

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2007.09.052

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title = "Novel synthetic ligands for targeted PET imaging and radiotherapy of copper",

abstract = "Novel ligands, NBEA, NBPA, NETA, NE3TA, and NE3TA-Bn, were synthesized and evaluated as potential chelators of copper radioisotopes for use in targeted positron emission tomography (PET) imaging or radiation therapy. The new ligands were radiolabeled with 64Cu, and in vitro stability of the radiolabeled complexes was assessed in rat serum. Serum stability results suggest that among the ligands tested, NETA, NE3TA, and NE3TA-Bn form stable complexes with 64Cu.",

keywords = "Cu-64, Macrocyclic ligands, PET imaging, Serum stability, Synthetic chelates, Targeted radiotherapy",

author = "Chong, {Hyun Soon} and Santosh Mhaske and Mai Lin and Sankar Bhuniya and Song, {Hyun A.} and Brechbiel, {Martin W.} and Xiankai Sun",

note = "Funding Information: This research was supported in part by the Intramural Research Program of the NIH, National Cancer Institute, Center for Cancer Research.",

year = "2007",

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doi = "10.1016/j.bmcl.2007.09.052",

language = "English (US)",

volume = "17",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - Novel synthetic ligands for targeted PET imaging and radiotherapy of copper

AU - Chong, Hyun Soon

AU - Mhaske, Santosh

AU - Lin, Mai

AU - Bhuniya, Sankar

AU - Song, Hyun A.

AU - Brechbiel, Martin W.

AU - Sun, Xiankai

N1 - Funding Information: This research was supported in part by the Intramural Research Program of the NIH, National Cancer Institute, Center for Cancer Research.

PY - 2007/11/15

Y1 - 2007/11/15

N2 - Novel ligands, NBEA, NBPA, NETA, NE3TA, and NE3TA-Bn, were synthesized and evaluated as potential chelators of copper radioisotopes for use in targeted positron emission tomography (PET) imaging or radiation therapy. The new ligands were radiolabeled with 64Cu, and in vitro stability of the radiolabeled complexes was assessed in rat serum. Serum stability results suggest that among the ligands tested, NETA, NE3TA, and NE3TA-Bn form stable complexes with 64Cu.

AB - Novel ligands, NBEA, NBPA, NETA, NE3TA, and NE3TA-Bn, were synthesized and evaluated as potential chelators of copper radioisotopes for use in targeted positron emission tomography (PET) imaging or radiation therapy. The new ligands were radiolabeled with 64Cu, and in vitro stability of the radiolabeled complexes was assessed in rat serum. Serum stability results suggest that among the ligands tested, NETA, NE3TA, and NE3TA-Bn form stable complexes with 64Cu.

KW - Cu-64

KW - Macrocyclic ligands

KW - PET imaging

KW - Serum stability

KW - Synthetic chelates

KW - Targeted radiotherapy

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JO - Bioorganic and Medicinal Chemistry Letters

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IS - 22

ER -

Novel synthetic ligands for targeted PET imaging and radiotherapy of copper

Abstract

Keywords

ASJC Scopus subject areas

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