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Modular synthesis and post-modification of novel bifunctional dendrons

Tulli, Ludovico and Pintassilgo Miranda, Daniela and Lee, Cameron and Sullivan, Yang and Grotzfeld, Robert and Hollingworth, Greg and 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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