Synthesis, antitumor activity, and chemical properties of silaplatin and related platinum(II) and platinum(IV) complexes derived from .beta.-silyl amines
作者:Wayne K. Anderson、Ravindra Kasliwal、D. Michael Houston、Yueh-sha Wang、Ven L. Narayanan、Rudiger D. Haugwitz、Jacqueline Plowman
DOI:10.1021/jm00019a008
日期:1995.9
cyclic complexes 2a ("silaplatin") and its Pt(IV) analogue, 2b, were very active against L1210 leukemia in vivo. Both the platinum (II) complex 2a and the platinum (IV) complex 2b produced a significant number of cures over the dose range 10-40 mg/kg. The platinum (II) complex 2a, silaplatin, was very active in vivo against an L1210 leukemia subline that was resistant to cisplatin; 2a was also active
制备了衍生自β-甲硅烷基取代的胺的铂(II)和铂(IV)配合物。测量所选复合物在水和生理盐水中的溶解度,并通过HPLC测定β-硅对复合物在水溶液中反应性的影响。将所选择的甲硅烷基络合物的稳定性与碳类似物进行比较。环状复合物2a(“ silaplatin”)及其Pt(IV)类似物2b在体内对L1210白血病具有很高的活性。铂(II)配合物2a和铂(IV)配合物2b在10-40 mg / kg的剂量范围内均产生了大量固化剂。铂(II)配合物2a硅铂在体内对抵抗顺铂的L1210白血病亚系具有非常高的活性。腹膜内注射2a时,对植入ic的L1210也有效。合成了环丁烷二羧酸配合物3c; m / z为1。该复合物对顺铂敏感和耐药的L1210白血病均具有活性,但效力不及类似的二氯化合物2a。合成了无环铂(II)和铂(IV)配合物1a,b,出乎意料地发现其在体内对L1210白血病无活性。制备了更多的亲脂性