新型低毒水溶性铂（II）配合物的小鼠抗肿瘤活性
Murine anti-tumor activity of new water soluble platinum(II) complexes with reduced toxicity.
作者信息
Talebian A H, Bensely D, Schein P S, Green D
机构信息
Department of Chemistry, Georgetown University, Washington, DC 20057.
出版信息
Anticancer Drug Des. 1990 Nov;5(4):371-8.
A series of new water soluble sugar and non-sugar containing platinum(II) complexes was synthesized and evaluated for effects of the sugar moiety on water solubility, anti-tumor activity, and acute leukopenia. When tested in vivo against the murine P388 and L1210 leukemias at LD10/maximally effective doses, the compound cis-[(gluconylamino)malonato-O,O'](1R,2R-cyclohexanediami ne-N,N')platinum (II), R,RG-AMP produced comparable or superior anti-tumor activity to cisplatin, carboplatin, and tetraplatin. Efficacy was also demonstrated for the L1210/DDP (cisplatin-resistant) leukemia. Further, R,R-G-AMP is non-nephrotoxic and produces less leukopenia than cisplatin, carboplatin, and tetraplatin.
合成了一系列新型的含铂（II）的水溶性糖和非糖配合物，并评估了糖部分对水溶性、抗肿瘤活性和急性白细胞减少症的影响。当以LD10/最大有效剂量在体内针对小鼠P388和L1210白血病进行测试时，化合物顺式 - [（葡糖氨酰氨基）丙二酸 - O，O']（1R，2R - 环己二胺 - N，N'）铂（II），R，R - G - AMP产生的抗肿瘤活性与顺铂、卡铂和四铂相当或更优。对L1210/DDP（顺铂耐药）白血病也显示出疗效。此外，R，R - G - AMP无肾毒性，且比顺铂、卡铂和四铂产生的白细胞减少症更少。
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