Issue 11, 2019

Modular synthesis and modification of novel bifunctional dendrons

Abstract

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 the PMBC culture.

Graphical abstract: Modular synthesis and modification of novel bifunctional dendrons

Supplementary files

Article information

Article type
Paper
Submitted
30 Nov 2018
Accepted
16 Jan 2019
First published
23 Jan 2019

Org. Biomol. Chem., 2019,17, 2906-2912

Modular synthesis and modification of novel bifunctional dendrons

L. G. Tulli, D. Miranda, C. C. Lee, Y. Sullivan, R. Grotzfeld, G. Hollingworth, R. Kneuer and A. S. Karpov, Org. Biomol. Chem., 2019, 17, 2906 DOI: 10.1039/C8OB02988A

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