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Gold (I)-Based Compounds and their Potential as Chemo- and Targeted- therapeutics for Renal and Breast Cancer

Osteguna, Abuztuak 08, 2019 - 12:00
Donostia International Physics Center
Maria Contel, Brooklyn College, The City University of New York
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Gold compounds are emerging as promising anticancer chemotherapeutics with a gold(I) compound Auranofin (a thiolate containing the [AuPEt3]+ fragment) being evaluated in clinical trials. Our group at Brooklyn College has reported on the preparation of heterometallic complexes containing titanocenes [TiCp2] or ruthenium(II) arene derivatives [RuCl2(p-cymene)(dppm)] and gold(I)-phosphane or gold(I)-N-heterocyclic NHC-carbene fragments and their potential as chemotherapeutics against renal or colorectal cancers (including studies of their efficacy in vivo, pharmacokinetics, histopathology and mechanisms). We will provide a brief overview on this topic. We are also working on strategies for the delivery of metal-based drugs so that they can be efficiently released at the specific tumor site to improve selectivity, bioavailability and blood circulation times. We will report on delivery vehicles for gold(I)-based cytotoxic agents (containing phosphanes and NHC-carbene ligands) consisting on: a) “smart” peptide nanocarriers, and b) antibodies such as trastuzumab. We will describe synthetic strategies to obtain antibody-drug conjugates and to encapsulate gold compounds in MMP-9 responsive peptide-based nanocarriers. Results for cellular viability assays in human renal and breast cancer cell lines and non-cancerous cell lines to highlight the tumor targeting properties of these systems will be discussed.
Host: Luca Salassa

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