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Title: Rapid insertion of bismuth radioactive isotopes into texaphyrin in aqueous media

Abstract

Radioisotopes 213Bi and 207Bi were successfully inserted into a water-soluble and tumor-targeting texaphyrin ligand. The reaction with 207Bi(OAc) 3 proceeds in about 15 min in aqueous media without the use of any organic base. The Bi(III) texaphyrin complex formed (3) is stable in aqueous media even in the presence of an excess of competitive chelators (EDTA or citric acid), as well as in human blood plasma. Finally, these results validate texaphyrins as potential candidates for coordinating bismuth radionuclides and set the stage for their use in targeted alpha therapy (TAT).

Authors:
 [1];  [2];  [2];  [2];  [2];  [1]
  1. Univ. of Texas, Austin, TX (United States). Dept. of Chemistry
  2. Los Alamos National Lab. (LANL), Los Alamos, NM (United States)
Publication Date:
Research Org.:
Los Alamos National Lab. (LANL), Los Alamos, NM (United States); Univ. of Texas, Austin, TX (United States)
Sponsoring Org.:
USDOE Office of Science (SC), Basic Energy Sciences (BES) (SC-22); LANL Laboratory Directed Research and Development (LDRD) Program; Robert A. Welch Foundation (United States)
OSTI Identifier:
1484672
Report Number(s):
LA-UR-18-31066
Journal ID: ISSN 1088-4246
Grant/Contract Number:  
89233218CNA000001; FG02-01ER15186; F-0018
Resource Type:
Journal Article: Accepted Manuscript
Journal Name:
Journal of Porphyrins and Phthalocyanines
Additional Journal Information:
Journal Volume: 21; Journal Issue: 12; Journal ID: ISSN 1088-4246
Publisher:
World Scientific
Country of Publication:
United States
Language:
English
Subject:
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY; bismuth radioisotopes; targeted alpha-emitter therapy; texaphyrin

Citation Formats

Thiabaud, Grégory, Radchenko, Valery, Wilson, Justin J., John, Kevin D., Birnbaum, Eva R., and Sessler, Jonathan L. Rapid insertion of bismuth radioactive isotopes into texaphyrin in aqueous media. United States: N. p., 2017. Web. doi:10.1142/S1088424617500870.
Thiabaud, Grégory, Radchenko, Valery, Wilson, Justin J., John, Kevin D., Birnbaum, Eva R., & Sessler, Jonathan L. Rapid insertion of bismuth radioactive isotopes into texaphyrin in aqueous media. United States. doi:10.1142/S1088424617500870.
Thiabaud, Grégory, Radchenko, Valery, Wilson, Justin J., John, Kevin D., Birnbaum, Eva R., and Sessler, Jonathan L. Sun . "Rapid insertion of bismuth radioactive isotopes into texaphyrin in aqueous media". United States. doi:10.1142/S1088424617500870. https://www.osti.gov/servlets/purl/1484672.
@article{osti_1484672,
title = {Rapid insertion of bismuth radioactive isotopes into texaphyrin in aqueous media},
author = {Thiabaud, Grégory and Radchenko, Valery and Wilson, Justin J. and John, Kevin D. and Birnbaum, Eva R. and Sessler, Jonathan L.},
abstractNote = {Radioisotopes 213Bi and 207Bi were successfully inserted into a water-soluble and tumor-targeting texaphyrin ligand. The reaction with 207Bi(OAc)3 proceeds in about 15 min in aqueous media without the use of any organic base. The Bi(III) texaphyrin complex formed (3) is stable in aqueous media even in the presence of an excess of competitive chelators (EDTA or citric acid), as well as in human blood plasma. Finally, these results validate texaphyrins as potential candidates for coordinating bismuth radionuclides and set the stage for their use in targeted alpha therapy (TAT).},
doi = {10.1142/S1088424617500870},
journal = {Journal of Porphyrins and Phthalocyanines},
issn = {1088-4246},
number = 12,
volume = 21,
place = {United States},
year = {2017},
month = {12}
}

Journal Article:
Free Publicly Available Full Text
Publisher's Version of Record

Citation Metrics:
Cited by: 1 work
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Figures / Tables:

Scheme 1. Scheme 1.: Protocols for metallation of texaphyrin macrocycles. Method 1: Stepwise strategy (“onepot”) that consists in oxidizing first using a ferrocenium salt to form as an intermediate (isolable species), and then inserting the metallic ion Bi3+ to form complex; Method 2 (shunting arrow on the left side): Concerted strategy usingmore » O2 as the oxidizing agent.« less

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Works referenced in this record:

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    Figures/Tables have been extracted from DOE-funded journal article accepted manuscripts.