Ruthenium polypyridyl complexes that induce mitochondria-mediated apoptosis in cancer cells.

Department of Chemistry, Jinan University, Guangzhou 510632, People's Republic of China.
Inorganic Chemistry (Impact Factor: 4.59). 07/2010; 49(14):6366-8. DOI: 10.1021/ic100277w
Source: PubMed

ABSTRACT The limitations of cisplatin-based chemotherapy, including high toxicity, undesirable side effects, and drug resistance, have motivated extensive investigations into alternative metal-based cancer therapies. Ruthenium (Ru) possesses several favorable properties suited to rational anticancer drug design and biological applications. In the present study, we synthesized a series of ruthenium polypyridyl complexes containing N,N-chelating ligands, examined their anticancer activities, and elucidated the molecular mechanisms through which they caused the cancer cell death. The results demonstrated that [Ru(phen)(2)-p-MOPIP](PF(6))(2).2H(2)O (RuPOP), a complex with potent antiproliferative activity, is able to induce mitochondria-mediated and caspase-dependent apoptosis in human cancer cells. On the basis of these results, we suggest that RuPOP may be a candidate for further evaluation as a chemopreventive and chemotherapeutic agent for human cancers, especially for melanoma.

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