Ruthenium(II)-Arene RAPTA Type Complexes Containing Curcunnin and Bisdemethoxycurcumin Display Potent and Selective Anticancer Activity
Pettinari, Riccardo; Marchetti, Fabio; Condello, Francesca; Pettinari, Claudio; Lupidi, Giulio; Scopelliti, Rosario; Mukhopadhyay, Suman; Riedel, Tina; Dyson, Paul J.
2014

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Abstract

A series of novel ruthenium(II) arene RAPTA type derivatives (arene = cymene, hexamethylbenzene) containing curcumin-based ligands (curcH = curcumin, bdcurcH = bisdemethoxycurcumin) and PTA (1,3,5-triaza-7-phosphaadamantane) have been synthesized and fully characterized. The solid-state structures of [Ru(cym)(curc)-(PTA)][SO3CF3], [Ru(hmb)(curc)(PTA)] [SO3CF3], and [Ru(hmb)(bdcurc)(PTA)]-[SO3CF3] have been determined by single-crystal X-ray diffraction. The antitumor activity of the complexes has been evaluated in vitro against human ovarian carcinoma cells (A2780 and A2780cisR), as well as against nontumorous human embryonic kidney (HEK293) cells. The correlation of the cytotoxicity upon switching the curcumin-based ligands, i.e. curcumin vs bisdemethoxycurcumin, is not straightforward. In contrast, the PTA ligand greatly enhances the activity and selectivity of ruthenium compounds in comparison to previously reported compounds.

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Title Ruthenium(II)-Arene RAPTA Type Complexes Containing Curcunnin and Bisdemethoxycurcumin Display Potent and Selective Anticancer Activity
Author(s) Pettinari, Riccardo ; Marchetti, Fabio ; Condello, Francesca ; Pettinari, Claudio ; Lupidi, Giulio ; Scopelliti, Rosario ; Mukhopadhyay, Suman ; Riedel, Tina ; Dyson, Paul J.
Published in Organometallics
Pagination 7
Volume 33
Issue 14
Pages 3709-3715
Date 2014
ISSN 0276-7333
DOI https://doi.org/10.1021/om500317b
Other identifier(s) View record in Web of Science
Laboratories LCOM
Record Appears in Scientific production and competences > SB - School of Basic Sciences > ISIC - Institute of Chemical Sciences and Engineering > LCOM - Laboratory of Organometallic and Medicinal Chemistry
Peer-reviewed publications
Work produced at EPFL
Journal Articles
Published
Record creation date 2014-08-29

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