Rationalization of monomer/cyclotrimer chemistry of coinage metals azolate compounds leading to unexpected biological properties Rossana Galassi School of Science and Technology, Chemistry Division, Camerino University, Via Sant’ Agostino, 1 62032 Italy. E-mail: rossana.galassi@unicam.it Crystal structures of cyclic trinuclear complexes of the d10 monovalent coinage metals are fascinating for their elegant self-assembly, their supramolecular stackings based on non-classic chemical bonding, and for their remarkably - rich optoelectronic properties. The significance of this class of complexes embraces cross-sectional chemistry areas, including metalloaromaticity, metallophilic bondings, supramolecular assemblies, M-M bonded excimers and exciplexes, and host/guest chemistry. Moreover, this class of complexes are surprising for their fascinating luminescence properties and their acid/base behavior.[1] Their synthesis proceeds by combining azolate salts with coinage metal precursors, where the departure of a leaving group i. e. PPh3, Me2S or the treatment with the M2O affords to cyclic rearrangements. However, it is possible to modulate the syntheses and the properties of the final products by changing the susbstituents in the azolate. By introducing withdrawing groups such as CF3, NO2, Cl, CN, mononuclear derivatives can be obtained showing solubility properties in aqueous media: these latter azolate gold(I) phosphane derivatives were found to be good candidate for biological studies. Azolate gold(I) phosphane compounds resulted to be cytotoxic on the regards of many panel of cancer cells, in addition to cis-platin resistant cells.[2] Moreover, they inhibit pivotal enzymes, such as the seleno dependent ThioredoxinaReductase (TrxR),[2]and an enzyme involved in DNA synthesis such as DeHydroFolateReductase [3] On these new azolate gold(I) phosphane compounds different cell viability assays (MTT assays) were performed on a human in vitro model of HER2-overexpressing breast cancer: SKBR-3 cells. After this preliminary screening, the most promising and effective compounds were selected to extend the study on A17 cell line, a murine preclinical model of Basal Like Breast Cancer (BLBC).[4] In this seminar, the chemistry, the characterization and the biological studies with the aforementioned azolate compounds will be presented. Leave one line blank [1] R. Galassi et al. Comm. Inorg. Chem., 2015 submitted. [2] R. Galassi et al., Dalton Trans., 2012, (41), pp 5307-5318. [3] R. Galassi et al., Dalton Trans., 2015, (44), pp 3043-3056. [4] M. Galiè et al., Carcinogenesis , 2005, (11), pp 1868-1

Rationalization of monomer/cyclotrimer chemistry of coinage metals azolate compounds leading to unexpected biological properties

GALASSI, Rossana
2015-01-01

Abstract

Rationalization of monomer/cyclotrimer chemistry of coinage metals azolate compounds leading to unexpected biological properties Rossana Galassi School of Science and Technology, Chemistry Division, Camerino University, Via Sant’ Agostino, 1 62032 Italy. E-mail: rossana.galassi@unicam.it Crystal structures of cyclic trinuclear complexes of the d10 monovalent coinage metals are fascinating for their elegant self-assembly, their supramolecular stackings based on non-classic chemical bonding, and for their remarkably - rich optoelectronic properties. The significance of this class of complexes embraces cross-sectional chemistry areas, including metalloaromaticity, metallophilic bondings, supramolecular assemblies, M-M bonded excimers and exciplexes, and host/guest chemistry. Moreover, this class of complexes are surprising for their fascinating luminescence properties and their acid/base behavior.[1] Their synthesis proceeds by combining azolate salts with coinage metal precursors, where the departure of a leaving group i. e. PPh3, Me2S or the treatment with the M2O affords to cyclic rearrangements. However, it is possible to modulate the syntheses and the properties of the final products by changing the susbstituents in the azolate. By introducing withdrawing groups such as CF3, NO2, Cl, CN, mononuclear derivatives can be obtained showing solubility properties in aqueous media: these latter azolate gold(I) phosphane derivatives were found to be good candidate for biological studies. Azolate gold(I) phosphane compounds resulted to be cytotoxic on the regards of many panel of cancer cells, in addition to cis-platin resistant cells.[2] Moreover, they inhibit pivotal enzymes, such as the seleno dependent ThioredoxinaReductase (TrxR),[2]and an enzyme involved in DNA synthesis such as DeHydroFolateReductase [3] On these new azolate gold(I) phosphane compounds different cell viability assays (MTT assays) were performed on a human in vitro model of HER2-overexpressing breast cancer: SKBR-3 cells. After this preliminary screening, the most promising and effective compounds were selected to extend the study on A17 cell line, a murine preclinical model of Basal Like Breast Cancer (BLBC).[4] In this seminar, the chemistry, the characterization and the biological studies with the aforementioned azolate compounds will be presented. Leave one line blank [1] R. Galassi et al. Comm. Inorg. Chem., 2015 submitted. [2] R. Galassi et al., Dalton Trans., 2012, (41), pp 5307-5318. [3] R. Galassi et al., Dalton Trans., 2015, (44), pp 3043-3056. [4] M. Galiè et al., Carcinogenesis , 2005, (11), pp 1868-1
2015
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11581/387025
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