title: Inorganic mesoporous silicas as vehicles of two novel anthracene-based ruthenium metalloarenes.
abstract: Two novel anthracene-based half-sandwich organometallic Ru(II) compounds, namely, [Ru(p-cymene)(L1)Cl2] (1) and [Ru(p-cymene)(L2)Cl2] (2) (L1=1-(anthracen-9-yl)-N-(pyridin-3-ylmethyl)methanamine; L2=1-(anthracen-9-yl)-N-(pyridin-4-ylmethyl)methanamine) have been synthesized and characterized. We demonstrate that the fluorescence properties of these complexes are highly affected by the linking position of the anthracene unit, as only 2 shows fluorescence emission in the blue region. Regarding their biological activity, both ruthenium metallodrugs show interaction with different biological targets such as S-donor amino acids (cysteine) and proteases (cysteine cathepsin B). Moreover, 1 and 2 show in vitro cytotoxicity against HL-60 cancer cell line (IC50=84.5 and 87.0μM for 1 and 2, respectively), with cell death occurring via apoptosis. Further studies have shown that diffusion into cells is the main mechanism of metallodrug uptake. Finally, as a proof of concept, these ruthenium complexes have been successfully encapsulated into MCM-41 and SBA-15 mesoporous silicas using two different incorporation strategies (impregnation and grinding).
authors.affiliation: Department of Inorganic Chemistry, University of Granada, Av. Fuentenueva S/N, 18071, Granada, Spain.
authors.forename: Sara
authors.initials: S
authors.lastname: Rojas
authors.affiliation: Department of Inorganic Chemistry, University of Granada, Av. Fuentenueva S/N, 18071, Granada, Spain.
authors.forename: Francisco J
authors.initials: FJ
authors.lastname: Carmona
authors.affiliation: Department of Inorganic Chemistry, University of Granada, Av. Fuentenueva S/N, 18071, Granada, Spain. Electronic address: ebaream@ugr.es.
authors.forename: Elisa
authors.initials: E
authors.lastname: Barea
authors.affiliation: Department of Inorganic Chemistry, University of Granada, Av. Fuentenueva S/N, 18071, Granada, Spain. Electronic address: crmaldonado@ugr.es.
authors.forename: Carmen R
authors.initials: CR
authors.lastname: Maldonado
mesh_terms: D000873:Anthracenes / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D003603:Cytotoxins / Q000737:chemistry / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry / Q000494:pharmacology; D018922:HL-60 Cells; D006801:Humans; D016062:Porosity; D012428:Ruthenium / Q000737:chemistry / Q000494:pharmacology; D012822:Silicon Dioxide / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000873:Anthracenes; D003603:Cytotoxins; D004337:Drug Carriers; D012822:Silicon Dioxide; D012428:Ruthenium
keywords: Cathepsin inhibition; Drug encapsulation; Fluorescence; MCM-41; Ruthenium metallodrug; SBA-15