Journal
MOLECULAR PHARMACEUTICS
Volume 18, Issue 1, Pages 65-73Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.molpharmaceut.0c00892
Keywords
phosphorus dendrimers; Cu(II) complexes; in vitro and in vivo antiproliferative efficacy
Funding
- PRC NSFC-CNRS 2019 [21911530230, 199675]
- FCT-Fundacao para a Cie<^>ncia e a Tecnologia [UIDB/00674/2020, UIDP/00674/2020]
- ARDITI-Age<^>ncia Regional para o Desenvolvimento da Investigaao Tecnologia e Inovacao [M1420-01-0145-FEDER-000005-CQM+]
- ERANET EuroNanoMed III
- CNRS (France)
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Phosphorus dendrimers, with their versatility and customizability, have promising applications in biomedicine.
Dendrimers are macromolecules with well-defined, homogeneous, and monodispersed structures that form a branch-like structure. In general, they have a symmetric core, inner shells, and an outer shell. Over the past decade, metallodendritic architectures have developed into a new area in nanomedicine. Due to their versatility and facile customization, phosphorus dendrimers represent interesting platforms for biomedical applications. Metallo-conjugated phosphorus dendrimers have been developed within the dendrimer space, an important part of the chemical space. The first investigation was made using phosphorus dendrimers bearing copper(II) groups on their surface as the original anticancer drug candidates. The aim of this minireview is to present our powerful strategy to find and develop original multivalent copper(II)-conjugated phosphorus dendrimers. The most potent of them is G3 dendrimers with N-(pyridine-2-ylmethylene)ethanamine as the chelating motif complexed with Cu(II) (1G3-Cu), showing very good in vitro and in vivo antiproliferative efficacy. On the basis of these results, 1G3-Cu is a potential clinical candidate having progressed from hit to preclinical candidate status.
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