Wimmer F L, Wimmer S, Castan P, Cros S, Johnson N, Colacio-Rodrigez E
Laboratoire de Pharmacologie et de Toxicologie Fondamentales du CNRS, Toulouse, France.
Anticancer Res. 1989 May-Jun;9(3):791-3.
A range of palladium(II) complexes with chelating ligands were assayed for their antitumor activity against the tumors P388 and S180 in female mice. The complexes tested were [Pd(L)(ONO2)2] (L = 2,2'-bipyridyl,2-(aminoethyl)pyridine (aep), 2-(aminomethyl)pyridine (amp], [Pd(eth)Cl2] (eth = ethionine) and [Pd(dach)(Meorot)] (dach = trans-1,2-diaminocyclohexane, Meorot = dianion of 3-methylorotic acid). The complexes were administered in water except [Pd(dach)(Meorot)] which was a suspension in klucel. The LD0 values were greater than or equal to 100 mg/kg. None of the complexes were active against the P388 tumor. [Pd(L)ONO2)2] (L = aep, amp) showed marginal activity against S180, while [Pd(dach-)(Meorot)] had an optimal T/C of 267% at dose of 150 mg/kg with 2/10 survivors on day 60.
对一系列含有螯合配体的钯（II）配合物进行了测试，以评估它们对雌性小鼠体内P388和S180肿瘤的抗肿瘤活性。所测试的配合物包括[Pd(L)(ONO2)2]（L = 2,2'-联吡啶、2-(氨基乙基)吡啶（aep）、2-(氨基甲基)吡啶（amp））、[Pd(eth)Cl2]（eth = 乙硫氨酸）以及[Pd(dach)(Meorot)]（dach = 反式-1,2-二氨基环己烷，Meorot = 3-甲基乳清酸的二价阴离子）。除了[Pd(dach)(Meorot)]是在羟丙基纤维素中的悬浮液外，其他配合物均以水溶液形式给药。LD0值大于或等于100 mg/kg。所有配合物对P388肿瘤均无活性。[Pd(L)ONO2)2]（L = aep、amp）对S180显示出微弱活性，而[Pd(dach)(Meorot)]在150 mg/kg剂量下的最佳T/C为267%，在第60天有2/10的存活者。
