Ru-Based NSAIDs as Potential Anticancer Therapeutics

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Abstract

The use of metal-based species bearing existing pharmaceuticals as ligands—often resulting in enhanced bioactivity—represents an attractive strategy for the development of novel therapeutic formulations. In this context, five well-known non-steroidal anti-inflammatory drugs (NSAIDs) were employed to substitute both PPh3 and hydride ligands in [Ru(H)2(CO)(PPh3)3] (1), thereby selectively affording neutral κ2-(O,O)–chelate complexes in satisfactory yields via molecular hydrogen release. Among the obtained species, two complexes coordinating diclofenac (4) and aspirin (5) were further investigated by single-crystal X-ray diffraction (SCXRD). Preliminary biological studies were conducted on the ruthenium–salicylic acid species 2 and ibuprofen 6. The former showed promising antiproliferative activity against HeLa cancer cells, consistent with the well-established role of NSAID–ruthenium(II) complexes as a platform for the development of novel anticancer metallotherapeutics.

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