Synthesis of MRI Contrast Agents Derived from DOTAM-Gly-L-Phe-OH Incorporating a Disulfide Bridge: Conjugation to a Cell Penetrating Peptide and Preparation of a Dimeric Agent

Authors

Mojmír Suchý, The University of Western Ontario
Alex X. Li, Robarts Research Institute, The University of Western Ontario
Robert Bartha, Robarts Research Institute, The University of Western Ontario
Robert H. E. Hudson, The University of Western Ontario

Document Type

Article

Publication Date

9-15-2010

Journal

Bioorganic & Medicinal Chemistry Letters

Volume

20

Issue

18

First Page

5521

Last Page

5526

URL with Digital Object Identifier

http://dx.doi.org/10.1016/j.bmcl.2010.07.070

Abstract

A cell penetrating peptide conjugate and dimeric PARACEST MRI contrast agents, based on the DOTAM-Gly-L-Phe-OH scaffold have been prepared in moderate yields using diethyl azodicarboxylate (DEAD) or iodine-mediated disulfide bridge formation as a key step. Magnetic (PARACEST) properties of these agents have been evaluated.