Synthesis and antitumor activity of 1,2-diaminocyclohexane platinum(IV) complexes.
Synthesis and antitumor activity of 1,2-diaminocyclohexane platinum(IV) complexes.
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1,2-二氨基环己烷铂(IV)配合物的合成及其抗肿瘤活性。
DOI：
10.1016/0162-0134(94)85122-0
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发表时间：
1994
影响因子：
3.9
通讯作者：
Siddik,ZH
中科院分区：
文献类型：
--
作者：
Khokhar,AR;al-Baker,S;Siddik,ZH
一系列 DACH-PtIV(X)2Y 型铂 (IV) 络合物的合成、表征和抗肿瘤活性（其中 DACH = 反式-dl、或反式-1-1,2-二氨基环己烷，X = OH 或 Cl，Y = 草酸根、丙二酸、甲基丙二酸、tartronato、酮丙二酸、1,1-环丙烷二羧基，或这些复合物已通过元素分析、HPLC、红外和 195 Pt NMR 光谱技术进行了表征。这些复合物具有良好的体外细胞毒活性（IC50= 0.14–7.6 μg/ml），并且在体内对白血病 L1210 细胞具有高度活性（%T/C = 152− > 600，顺铂 = 218）此外，选择用于进一步评估的类似物还表现出针对 B16 黑色素瘤（%T/C = 309）、M5076 网状肉瘤（100% 治愈）和顺铂耐药 L1210/DDP（%T/C = 217）细胞系的优异体内抗肿瘤活性。
The synthesis, characterization, and antitumor activity of a series of platinum(IV) complexes of the type DACH-PtIV(X)2Y (where DACH =trans-dl, ortrans-1-1,2-diaminocyclohexane, X = OH or Cl, and Y = oxalato, malonato, methylmalonato, tartronato, ketomalonato, 1,1-cyclopropanedicarboxylato, or 1,1-cyclobutanedicarboxylato, are described. These complexes have been characterized by elemental analysis, HPLC, and infrared and195Pt NMR spectroscopic techniques. The complexes had good in vitro cytotoxic activity (IC50= 0.14–7.6 μg/ml) and were highly active in vivo against leukemia L1210 cells (%T/C = 152− > 600, cisplatin = 218). In addition, excellent in vivo antitumor activities against B16 melanoma (%T/C = 309), M5076 reticulosarcoma (100% cures) and cisplatin-resistant L1210/DDP (%T/C = 217) cell lines were also exhibited by an analog selected for further evaluation.