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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

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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.

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