Ruthenium(II)鈥揂rene RAPTA Type Complexes Containing Curcumin and Bisdemethoxycurcumin Display Potent and Selective Anticancer Activity

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• 作者：Riccardo Pettinari ; Fabio Marchetti ; Francesca Condello ; Claudio Pettinari ; Giulio Lupidi ; Rosario Scopelliti ; Suman Mukhopadhyay ; Tina Riedel ; Paul J. Dyson
• 刊名：Organometallics
• 出版年：2014
• 出版时间：July 28, 2014
• 年：2014
• 卷：33
• 期：14
• 页码：3709-3715
• 全文大小：338K
• ISSN：1520-6041

文摘

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.