Synthesis and Antitumor Activity of Pt(II) Complexes of Benzyl‐1,2‐diaminoethane Ligands

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Abstract
Twelve new diamine ligands are synthesized and characterized in which a benzyl group and another vicinal substituent or a benzyl group, a 4‐Cl‐benzyl group, and a 4‐MeO‐benzyl group, respectively, and two other geminal substituents are attached to the 1,2‐diaminoethane skeleton. The diamine ligands are transformed into the dichloroplatinum(II) complexes. The chloride ligands of four complexes are replaced by the lactate anion, α‐Cyclodextrin and polyvinylpyrrolidone are used to increase the water solubility of the Pt(II) complexes. The antitumor activity of the Pt(II) complexes is tested towards the P388 leukemia. The compounds with small alkyl substituents show antitumor activities which are much higher than the antitumor activity of cis‐platinum. Compared to the insoluble dichloro complexes, the lactate complexes and the formulations with α‐cyclodextrin and polyvinylpyrrolidone exhibit good water solubility, and no decrease of the antitumor activity is observed.

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