4.7 Article

Acridine-decorated cyclometallated gold(III) complexes: synthesis and anti-tumour investigations

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DALTON TRANSACTIONS
卷 47, 期 38, 页码 13523-13534

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c8dt02507j

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  1. European Research Council
  2. ERC [338944-GOCAT]

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(C boolean AND N) and (C boolean AND N boolean AND C) cyclometalated Au(iii) represent a highly promising class of potential anticancer agents. We report here the synthesis of seven new cyclometalated Au(iii) complexes with five of them bearing an acridine moiety attached via (N boolean AND O) or (N boolean AND N) chelates, acyclic amino carbenes (AAC) and N-heterocyclic carbenes (NHC). The antiproliferative properties of the different complexes were evaluated in vitro on a panel of cancer cells including leukaemia, lung and breast cancer cells. We observed a trend between the cytotoxicity and the intracellular gold uptake of some representative compounds of the series. Some of the acridine-decorated complexes were demonstrated to interact with ds-DNA using FRET-melting techniques.

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