[DL-1,2-双(2-羟基苯基)乙二胺]二氯铂(II)，一种用于治疗卵巢癌的新化合物。
[DL-1,2-bis(2-hydroxyphenyl)ethylenediamine]dichloroplatinum(II), a new compound for the therapy of ovarian cancer.
作者信息
Müller R, Gust R, Bernhardt G, Keller C, Schönenberger H, Seeber S, Osieka R, Eastman A, Jennerwein M
机构信息
Institut für Pharmazie, Lehrstuhl Pharmazeutische Chemie II, Universität Regensburg, Federal Republic of Germany.
出版信息
J Cancer Res Clin Oncol. 1990;116(3):237-44. doi: 10.1007/BF01612897.
The synthesis of diastereoisomeric [1,2-bis(2-hydroxyphenyl)ethylenediamine]dichloroplatinum(II) complexes, DL-3-PtCl2 and meso-3-PtCl2, and their evaluation on the hormone-independent, human MDA-MB231 breast cancer cell line, on the cisplatin-sensitive and -resistant L1210 leukemia cell line, on the cisplatin-resistant human NIH:OVCAR 3 ovarian cancer cell line, on the P-388 leukemia of the mouse and on the cisplatin-sensitive and -resistant Ehrlich ascites tumor of the mouse are described. On all tumor models DL-3-PtCl2 produces a marked inhibitory effect. The diastereoisomer meso-3-PtCl2 is less active and more toxic. It is striking that DL-3-PtCl2 leads to a pronounced inhibition of all cisplatin-resistant tumors. At non-toxic concentrations DL-3-PtCl2 produces cytocidal effects on the NIH:OV-CAR 3 cell line. Therefore DL-3-PtCl2 is of interest for further evaluation for the therapy of ovarian cancer.
非对映异构的[1,2 - 双(2 - 羟基苯基)乙二胺]二氯铂(II)配合物DL - 3 - PtCl₂和内消旋 - 3 - PtCl₂的合成，以及它们对激素非依赖性人MDA - MB231乳腺癌细胞系、对顺铂敏感和耐药的L1210白血病细胞系、对顺铂耐药的人NIH:OVCAR 3卵巢癌细胞系、对小鼠P - 388白血病以及对小鼠顺铂敏感和耐药的艾氏腹水瘤的评估情况在此作了描述。在所有肿瘤模型中，DL - 3 - PtCl₂均产生显著的抑制作用。非对映异构体内消旋 - 3 - PtCl₂活性较低且毒性更大。引人注目的是，DL - 3 - PtCl₂对所有顺铂耐药肿瘤均有明显抑制作用。在无毒浓度下，DL - 3 - PtCl₂对NIH:OV - CAR 3细胞系产生杀细胞作用。因此，DL - 3 - PtCl₂对于卵巢癌治疗的进一步评估具有意义。
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