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Modular synthesis and post-modification of novel bifunctional dendrons

Tulli, Ludovico, Pintassilgo Miranda, Daniela, Lee, Cameron, Sullivan, Yang, Grotzfeld, Robert, Hollingworth, Greg, Kneuer, Rainer and Karpov, Alexei (2019) Modular synthesis and post-modification of novel bifunctional dendrons. Organic and biomolecular chemistry. ISSN 1477-0539; 1477-0520


Herein, we report the design and synthesis of two novel bifunctional dendrons bearing multiple amine termini at the periphery and an azide at the focal point. Copper-catalyzed alkyne-azide cycloaddition enabled modular dendritic scaffold assembly resulting in a first generation dendron carrying six amines and a second generation dendron carrying eighteen amines. Peripheral amines were labeled with multiple copies of a metal isotope, whereas the azide functionality at the focal point was employed in conjugation to a single anti-human CD4 antibody. We demonstrated that the highly monomeric first generation dendron-antibody conjugate selectively detected CD4+ T cells in PMBCs culture.

Item Type: Article
Date Deposited: 21 Feb 2019 00:45
Last Modified: 21 Feb 2019 00:45


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