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Motekaitis RJ, Rogers BE, Reichert DE, et al. Stability and Structure of Activated Macrocycles. Ligands with Biological Applications. Inorg Chem. 1996;35(13):3821-3827doi: 10.1021/ic960067g.
Motekaitis, R. J., Rogers, B. E., Reichert, D. E., Martell, A. E., & Welch, M. J. (1996). Stability and Structure of Activated Macrocycles. Ligands with Biological Applications. Inorganic chemistry, 35(13), 3821-3827. https://doi.org/10.1021/ic960067g
Motekaitis, Ramunas J., et al. "Stability and Structure of Activated Macrocycles. Ligands with Biological Applications." Inorganic chemistry vol. 35,13 (1996): 3821-3827. doi: https://doi.org/10.1021/ic960067g
Motekaitis RJ, Rogers BE, Reichert DE, Martell AE, Welch MJ. Stability and Structure of Activated Macrocycles. Ligands with Biological Applications. Inorg Chem. 1996 Jun 19;35(13):3821-3827. doi: 10.1021/ic960067g. PMID: 11666570.
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Inorg Chem. 1996 Jun 19;35(13):3821-3827. doi: 10.1021/ic960067g.

Stability and Structure of Activated Macrocycles. Ligands with Biological Applications.

Inorganic chemistry

Ramunas J. Motekaitis, Buck E. Rogers, David E. Reichert, Arthur E. Martell, Michael J. Welch

Affiliations

  1. Department of Chemistry, Texas A&M University, College Station, Texas 77843-3255, and The Edward Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, Missouri 63110.

PMID: 11666570 DOI: 10.1021/ic960067g

Abstract

Single p-toluic acid pendant groups were attached to 1,4,7,10,13-pentaazacyclopentadecane (15aneN5) and 1,4,8,11-tetraazacyclotetradecane (cyclam) to prepare bifunctional reagents for radiolabeling monoclonal antibodies with (64,67)Cu. The ligands are 1,4,7,10,13-pentaazacyclopentadecane-1-(alpha-1,4-toluic acid) (PCBA) and 1,4,8,11-tetraazacyclotetradecane-1-(alpha-1,4-toluic acid) (CPTA). For the parent macrocycles and their pendant arm derivatives, the 1:1 Cu(2+) complexes dissociate only below pH 2. At pH 0.0 and 25 degrees C the CPTA-Cu complex has a half-life toward complete dissociation of 24 days. A new approach was developed for the estimation of the Cu(2+) stability constant for the kinetically robust CPTA. All other formation constants were determined at 25.0 degrees C with batch spectrophotometric techniques. Potentiometric titrations were used to determine the protonation constants of the macrocyclic ligands as well as of the metal chelates. The protonation constants, stability constants, and pM's are discussed in terms of both molecular mechanics calculations and the ligands' potential applicability as copper(II) radiopharmaceuticals.

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