Synthesis and Relaxivity Studies of a DOTA-Based Nanomolecular Chelator Assembly Supported by an Icosahedral Closo-B122− -Core for MRI: A Click Chemistry Approach

Molecules

Lalit N. Goswami¹  Lixin Ma¹  Peter J. Kueffer¹  Satish S. Jalisatgi¹ 

[1] id="af1-molecules-18-09034">International Institute of Nano and Molecular Medicine, School of Medicine, University of Missouri, Columbia, MO 65211-3450, U

关键词: click reaction;    closo-boranes;    MRI contrast agents;    relaxivity;    gadolinium complexes;    DOTA;   

DOI  :  10.3390/molecules18089034

来源: mdpi

【 摘 要 】

An icosahedral closo-B₁₂²⁻ scaffold based nano-sized assembly capable of carrying a high payload of Gd³⁺-chelates in a sterically crowded configuration is developed by employing the azide-alkyne click reaction. The twelve copies of DO3A-t-Bu-ester ligands were covalently attached to an icosahedral closo-B₁₂²⁻ core via suitable linkers through click reaction. This nanomolecular structure supporting a high payload of Gd³⁺-chelate is a new member of the closomer MRI contrast agents that we are currently developing in our laboratory. The per Gd ion relaxivity (r₁) of the newly synthesized MRI contrast agent was obtained in PBS, 2% tween/PBS and bovine calf serum using a 7 Tesla micro MRI instrument and was found to be slightly higher (r₁ = 4.7 in PBS at 25 °C) compared to the clinically used MRI contrast agents Omniscan (r₁ = 4.2 in PBS at 25 °C) and ProHance (r₁ = 3.1 in PBS at 25 °C).

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.