Synthesis and antitumor activity of water-soluble 2-benzyl-1,2-diaminobutane-α-oxycarboxylatoplatinum(II) complexes
作者:Henri Brunner、Friedrich Maiterth、Barbara Treittinger
DOI:10.1016/s0020-1693(00)92348-x
日期:1992.8
2-diaminobutane-O,O′-lactatoplatinum(II), the different geometrical and optical isomers were separated. The antitumor activity of the platinum(II) complexes was examined in vitro towards the MDA-MB 231 breast cancer cell line and in vivo towards the P 388 leukemia of the CD2F1 mouse. Contrary to the insoluble dichloro complexes, the α-oxycarboxylatoplatinum(II) complexes exhibited good water solubility
合成并表征了九种新型水溶性铂(II)配合物。外消旋的(±)-2-苄基-1,2-二氨基丁烷或相应的对映异构体(+)-2-苄基-1,2-二氨基丁烷和(-)-2-苄基-1,2-二氨基丁烷用作氮螯合物配体。所得N,N'-2-苄基-1,2-二氨基丁烷二氯铂(II)配合物的氯化物离去基团被四种α-羟基羧酸的阴离子取代,以增加水溶性。作为α-羟基羧酸,使用乳酸,乙醇酸,扁桃酸和α-羟基异丁酸。对于N,N'-2-苄基-1,2-二氨基丁烷-O,O'-乳白铂(II),分离了不同的几何异构体和光学异构体。铂(II)配合物的抗肿瘤活性在体外针对MDA-MB 231乳腺癌细胞系进行了研究,并在体内针对CD2F1小鼠的P 388白血病进行了研究。与不溶性二氯配合物相反,α-氧基羧基铂(II)配合物表现出良好的水溶性,并具有很高的抗肿瘤活性。