Bitha P, Carvajal S G, Citarella R V, Delos Santos E F, Durr F E, Hlavka J J, Lang S A, Lindsay H L, Thomas J P, Wallace R E
American Cyanamid Company, Medical Research Division, Pearl River, New York 10965.
J Med Chem. 1989 Sep;32(9):2063-7. doi: 10.1021/jm00129a008.
[1,1-Cyclobutanedicarboxylato(2)-O,O'](1,3-dioxane-5,5-dimethan amine- N,N')platinum(II), 3a, a third generation, very water-soluble platinum complex, has been synthesized along with several of its analogues. All members of the new family contain a 1,3-dioxane or 1,3-dioxolane-1,3-diamine as their basic ligand, a moiety which contributes to their increased water solubility, and a bidentate acid ligand, which is responsible for their good stability. They were all easily crystallized and characterized by 1H NMR and elemental analysis, and the parent complex 3a was further characterized by 13C NMR. Their very desirable physical properties combined with their broad spectrum of antitumor activity and reduced toxicity make them good candidates of further development.
[1,1-环丁烷二甲酸根（2）-O，O']（1,3-二氧六环-5,5-二甲胺-N，N'）铂（II），即3a，一种第三代的、水溶性很强的铂配合物，已与其几种类似物一同合成出来。新系列的所有成员都含有一个1,3-二氧六环或1,3-二氧戊环-1,3-二胺作为其基本配体，这一部分有助于提高它们的水溶性，还有一个双齿酸配体，它赋予了它们良好的稳定性。它们都很容易结晶，并通过1H NMR和元素分析进行了表征，母体配合物3a还通过13C NMR进行了进一步表征。它们非常理想的物理性质，再加上其广泛的抗肿瘤活性谱和较低的毒性，使它们成为进一步开发的良好候选物。
