Synthesis and Relaxivity Studies of a DOTA-Based Nanomolecular Chelator Assembly Supported by an Icosahedral Closo-B122− -Core for MRI: A Click Chemistry Approach
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 c...
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MDPI AG
2013-07-01
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Series: | Molecules |
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Online Access: | http://www.mdpi.com/1420-3049/18/8/9034 |
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author | Satish S. Jalisatgi M. Frederick Hawthorne Peter J. Kueffer Lixin Ma Lalit N. Goswami |
author_facet | Satish S. Jalisatgi M. Frederick Hawthorne Peter J. Kueffer Lixin Ma Lalit N. Goswami |
author_sort | Satish S. Jalisatgi |
collection | DOAJ |
description | 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). |
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issn | 1420-3049 |
language | English |
last_indexed | 2024-12-22T01:43:07Z |
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spelling | doaj.art-9949368f7aab48b6b9e6d9739d2dc9e42022-12-21T18:43:08ZengMDPI AGMolecules1420-30492013-07-011889034904810.3390/molecules18089034Synthesis and Relaxivity Studies of a DOTA-Based Nanomolecular Chelator Assembly Supported by an Icosahedral Closo-B122− -Core for MRI: A Click Chemistry ApproachSatish S. JalisatgiM. Frederick HawthornePeter J. KuefferLixin MaLalit N. GoswamiAn 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).http://www.mdpi.com/1420-3049/18/8/9034click reactioncloso-boranesMRI contrast agentsrelaxivitygadolinium complexesDOTA |
spellingShingle | Satish S. Jalisatgi M. Frederick Hawthorne Peter J. Kueffer Lixin Ma Lalit N. Goswami 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 click reaction closo-boranes MRI contrast agents relaxivity gadolinium complexes DOTA |
title | Synthesis and Relaxivity Studies of a DOTA-Based Nanomolecular Chelator Assembly Supported by an Icosahedral Closo-B122− -Core for MRI: A Click Chemistry Approach |
title_full | Synthesis and Relaxivity Studies of a DOTA-Based Nanomolecular Chelator Assembly Supported by an Icosahedral Closo-B122− -Core for MRI: A Click Chemistry Approach |
title_fullStr | Synthesis and Relaxivity Studies of a DOTA-Based Nanomolecular Chelator Assembly Supported by an Icosahedral Closo-B122− -Core for MRI: A Click Chemistry Approach |
title_full_unstemmed | Synthesis and Relaxivity Studies of a DOTA-Based Nanomolecular Chelator Assembly Supported by an Icosahedral Closo-B122− -Core for MRI: A Click Chemistry Approach |
title_short | Synthesis and Relaxivity Studies of a DOTA-Based Nanomolecular Chelator Assembly Supported by an Icosahedral Closo-B122− -Core for MRI: A Click Chemistry Approach |
title_sort | synthesis and relaxivity studies of a dota based nanomolecular chelator assembly supported by an icosahedral closo b122 core for mri a click chemistry approach |
topic | click reaction closo-boranes MRI contrast agents relaxivity gadolinium complexes DOTA |
url | http://www.mdpi.com/1420-3049/18/8/9034 |
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