Heterofunctionalized Carbosilane Dendritic Systems: Bifunctionalized Dendrons as Building Blocks versus Statistically Decorated Dendrimers

“Click” chemistry based on thiol–ene synthetic protocols has been used to successfully bifunctionalize anionic carbosilane dendritic structures in two effective ways. The first consists of the formation of statistically heterofunctionalized dendrimers, the second being the synthesis of heterofunctionalized dendrons. Regarding the latter approach, a versatile and simple procedure has been developed for the synthesis of a library of anionic carbosilane dendrons. Taking into account the chemical diversity at the focal point for both neutral- and anionic-terminated dendrons, such as azide, alcohol, amine, bromine, carboxylic acid, and alkyne, these dendritic systems may act as building blocks to give more original dendritic architectures

Thiol-Ene Synthesis of Cationic Carbosilane Dendrons: a New Family of Synthons

A variety of neutral and cationic carbosilane dendrons containing a wide range of active groups, such as −N₃, −OH, −NH₂, and −SH, at the focal points were synthesized from carbosilane vinyl dendrons BrG_<i>n</i>V_<i>m</i> from generations 1–3 by substitution of the bromine atom at the focal point and functionalization of the vinyl groups via thiol-ene click chemistry with HS­(CH₂)₂NMe₂·HCl. These dendritic wedges were characterized by NMR, MS, and elemental analysis

Carbosilane Dendrimer 2G-NN16 Represses Tc17 Differentiation in Primary T CD8+ Lymphocytes

We studied changes in gene expression induced by the carbosilane dendrimer 2G-NN16 to evaluate their potential as a vehicle for gene therapy and as medication. Global gene expression profiles on CD8+ T lymphocytes reveal that ribosomal proteins are induced in the presence of 2G-NN16. IL17A and IL17F, the principal interleukins secreted by Tc17 cells, a subset of CD8+ T lymphocytes, were down-regulated when cultured in the presence of this dendrimer. Microarray results were confirmed by real time quantitative reverse transcriptase polymerase chain reaction (qRT-PCR). 2G-NN16 also showed a high potential for in vitro inhibition of Tc17 differentiation of CD8+ T lymphocytes in the presence of the Tc17 differentiation molecules IL6 and TGF-B1. These findings suggest that 2G-NN16 could facilitate drug delivery and may be used to treat inflammatory processes driven by Tc17 cells