Rapid insertion of bismuth radioactive isotopes into texaphyrin in aqueous media

Author:

Thiabaud Grégory1,Radchenko Valery2,Wilson Justin J.2,John Kevin D.2,Birnbaum Eva R.2,Sessler Jonathan L.1

Affiliation:

1. Department of Chemistry, The University of Texas at Austin, 105 East 24th Street, Stop A5300, Austin, TX, 78712-1224, USA

2. Los Alamos National Laboratory, P.O. Box 1663, Los Alamos, NM, 87545, USA

Abstract

Radioisotopes [Formula: see text]Bi and [Formula: see text]Bi were successfully inserted into a water-soluble and tumor-targeting texaphyrin ligand. The reaction with [Formula: see text]Bi(OAc)[Formula: see text] 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. These results validate texaphyrins as potential candidates for coordinating bismuth radionuclides and set the stage for their use in targeted alpha therapy (TAT).

Publisher

World Scientific Pub Co Pte Lt

Subject

General Chemistry

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