Claycamp H G, Shaw E I, Zimbrick J D
Radiat Res. 1986 May;106(2):141-6.
A piperidinyl-labeled platinum(II) complex, cis-Pt[2,2,6,6-tetramethyl-4-aminopiperidine-N-oxyl]2dichloride , is an ESR-traceable analog of the antitumor agent, cis-diamminedichloroplatinum(II), DDP. The toxicity of the analog (PDN-1) in Chinese hamster ovary (CHO) cells is 22 times less than that of the parent compound: D0 (where D0 = slope-1 of the straight-line portion of the survival curve) = 0.11 mM versus 0.0053 mM for 1.5-h treatments with PDN-1 and DDP, respectively. At PDN-1 doses that cause 10% killing when used alone, no statistically significant increase in cell killing of hypoxic, irradiated cells was observed. PDN-1 does not have significant dose-modifying properties but may be a useful probe to study platinum in mammalian cells.
一种哌啶基标记的铂(II)配合物,顺式-二氯[2,2,6,6-四甲基-4-氨基哌啶-N-氧基]铂(II),是抗肿瘤药物顺式二氯二氨铂(II)(DDP)的一种可通过电子自旋共振(ESR)追踪的类似物。该类似物(PDN-1)对中国仓鼠卵巢(CHO)细胞的毒性比母体化合物低22倍:D0(其中D0 = 存活曲线直线部分的斜率倒数)对于用PDN-1和DDP分别处理1.5小时而言,分别为0.11 mM和0.0053 mM。在单独使用时导致10%细胞杀伤的PDN-1剂量下,未观察到缺氧、受辐照细胞的细胞杀伤有统计学上的显著增加。PDN-1不具有显著的剂量修饰特性,但可能是研究哺乳动物细胞中铂的有用探针。