环戊二烯基氟尿嘧啶基钛（Ⅳ）、锆（Ⅳ）配合物的合成及其抗肿瘤活性的研究

Synthesis and Antitumor Activity of Cyclopentadienyl Titanium(Ⅳ),Zirconium(Ⅳ) Fluorouracil Complexes

用（ＲＣｐ）２ＭＣｌ２和（ＲＣｐ）ＴｉＣｌ３（Ｒ＝Ｈ，Ｍｅ；Ｍ＝Ｔｉ，Ｚｒ）分别与具有生物活性的２－甲氧基－５－氟尿嘧啶、２－甲硫基－５－氟尿嘧啶在甲苯溶剂中１１０℃下反应，合成了２０个未见报道的（ＲＣｐ）·Ｍ（Ｏｐｍ）２Ｃｌ、（ＲＣｐ）２Ｍ（ＯＰｍ）Ｃｌ和（ＲＣｐ）Ｍ（ＯＰｍ）Ｃｌ２（ＯＰｍ＝２－甲氧基－５－氟尿嘧啶基，２－甲硫基－５－氟尿嘧啶基）型钛锆配合物，这些配合物均经元素分析、１ＨＮＭＲ、ＩＲ光谱鉴定．初步动物试验表明，配合物１、４、１１、１４对小白鼠移植性艾氏腹水场的抑制作用居首，而配合物２、３、５、６、１２、１３、１５、１６次之，其它锆配合物几乎没有抑制作用。

Twenty of the 5-fluorouracil titanium(Ⅳ),zirconium(Ⅳ)complexes of type(RCp)M(Opm)2Cl,(RCp)2M(Opm)Cl and (RCp)Ti(Opm)Cl2(OPm=X=O,S) have been prepared by the reaction of dichloro bis(cyclopentadinyl)or(methylcyclopentadinyl)titanium and zirconium and trichlorocyclopentaclinyl or methylcy-clopentadienyl titanium with 2-methoxy-5-fluorouracil and 2-methylthio-5-fluorouracil, which have antitumor activities respectively in toluene at 110 ℃.All the complexes have been characterized by elementary analysis,1H NMR and IR spectra.The antitumor activities against Ehrlich ascites carcinoma in mice were observed.