Synthetic Route to Dinuclear Platinum(II) Complexes [{trans-PtCl(NH3)2}2(μ-L)]2+ (L = Aliphatic or Heterocyclic Diamine) as Potential Antitumor Agents, Exploiting the Mutual Activation of Hydroxido Ligands and Ammonium Groups

Chopard, Claude; Lenoir, Christine; Rizzato, Silvia; Vidal, Michel; Arpalahti, Jorma; Gabison, Laure; Albinati, Alberto; Garbay, Christiane; Kozelka, Jiří

doi:10.1021/ic801251k.s002

ic801251k_si_002.pdf (85.48 kB)

Synthetic Route to Dinuclear Platinum(II) Complexes [{trans-PtCl(NH₃)₂}₂(μ-L)]²⁺ (L = Aliphatic or Heterocyclic Diamine) as Potential Antitumor Agents, Exploiting the Mutual Activation of Hydroxido Ligands and Ammonium Groups

journal contribution

posted on 2008-10-20, 00:00 authored by Claude Chopard, Christine Lenoir, Silvia Rizzato, Michel Vidal, Jorma Arpalahti, Laure Gabison, Alberto Albinati, Christiane Garbay, Jiří Kozelka

A simple and efficient method for the synthesis of potentially antitumor-active dinuclear platinum complexes of the general formula [{trans-PtCl(NH₃)₂}₂(μ-L)]⁽ⁿ⁺²⁾⁺ (L = aliphatic or heterocyclic diamine; n = charge of L) is presented. The procedure is based on the mutual in situ activation of trans-[PtCl(OH)(NH₃)₂] and the linker L in the form of a diammonium salt. This synthetic pathway yielded the Farrell compound [{trans-PtCl(NH₃)₂}₂{μ-NH₂(CH₂)₆NH₂}]Cl₂ (BBR3005) in quantitative yield. Using the same procedure, we prepared the new pyrazolate-bridged compound [{trans-PtCl(NH₃)₂}₂(μ-pz)]Cl, determined its X-ray structure, and tested its cytotoxicity against three wild-type and one cisplatin-resistant cell lines.