Data Sheet 1_Active targeting towards bone cancer and metastases by pamidronate-bridged dinuclear platinum(II) complexes.pdf

Among nitrogen-containing BPs, pamidronate (PAM) is widely used for the management of cancer-related bone complications and has also been associated with antiproliferative and pro-apoptotic effects in several tumor models. These properties make PAM an attractive ligand for the development of potential bone-targeted anticancer agents, particularly in the context of primary bone tumors and bone metastases, which are difficult to treat and are frequently associated with severe pain and skeletal complications.

Platinum-based chemotherapeutics are effective anticancer agents, but their clinical use is often limited by poor tissue selectivity, systemic toxicity, and drug resistance. In this work, we report the synthesis and full characterization of two novel dinuclear platinum(II)–PAM complexes in which PAM acts as a bridging ligand between two platinum centers containing either an oxaliplatin-derived [Pt(1R,2R-diaminocyclohexane)]²⁺ unit or a kiteplatin-derived [Pt(cis-1,4-diaminocyclohexane)]²⁺ unit.