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J Med Chem. 2013 Feb 28;56(4):1782-6. doi: 10.1021/jm4000177. Epub 2013 Feb 19.

Structure-relaxivity relationships of serum albumin targeted MRI probes based on a single amino acid Gd complex.

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1
The Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, 149 Thirteenth Street, Suite 2301, Charlestown, Massachusetts 02129, United States.

Abstract

The Gd(III) complex of DO3A-N-α-aminopropionate, Gd(DOTAla), was used to generate a small library of putative MRI probes targeted to human serum albumin (HSA). Ten compounds were synthesized via multistep organic synthesis, and the corresponding Gd complexes were investigated for their affinity to HSA, lipophilicity, and relaxivity in the absence and presence of HSA. Negative charge and moderate lipophilicity correlate with increased HSA affinity and relaxivity.

PMID:
23391162
PMCID:
PMC3656968
DOI:
10.1021/jm4000177
[Indexed for MEDLINE]
Free PMC Article
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