The potential of gold (I) and (III) compounds as anticancer chemotherapeutics is now being unveiled. Gold(I)-phosphane or gold(I)-N-heterocyclic NHC-carbene complexes (like Auranofin in Chart 1) have shown promising results in advanced preclinical and clinical studies, while displaying a mode of action different from that of FDA approved platinum-based drugs. These gold(I) compounds serve as excellent building blocks for the synthesis of heterometallic complexes containing titanocenes [TiCp2] or ruthenium(II) arene derivatives [RuCl2(p-cymene)(dppm)]. We will discuss briefly the potential of these bimetallic Ti-Au and Ru-Au compounds against renal or prostate cancers (including studies of their efficacy in vivo, pharmacokinetics, histopathology and mechanisms). We will also report on delivery strategies for gold(I)-based cytotoxic agents in order to improve their selectivity, bioavailability and blood circulation times. We will describe the synthesis of bioconjugates based on gold(I) compounds and the monoclonal antibody Trastuzumab (gold-based antibody-drug conjugates). We will also report on the encapsulation of gold(I) anticancer agents in MMP-9 responsive peptide-based nanocarriers. MMP-9 is overexpressed in certain cancer cell lines and it can be used to cleave the nanopeptides releasing the gold payload in the tumor site. For these last two systems, we will provide cellular viability assays' results in human renal and breast cancer cell lines and non-cancerous cell lines to highlight their targeting properties.

Gold (I) anticancer agents: Building blocks for the synthesis of bimetallic compounds, bioconjugates and nanocarrier payloads. Preclinical studies

2019 Fall National Meeting

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