铂的配合物抗肿瘤作用。

Cancer chemotherapy reports Pub Date : 1975-05-01
R J Speer, H Ridgway, L M Hall, D P Stewart, K E Howe, D Z Lieberman, A D Newman, J M Hill
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引用次数: 0

摘要

Rosenberg和VanCamp首次报道了某些铂配位化合物的抑菌和抗肿瘤特性。这项开创性的工作导致了大量相关铂产品的合成和测试,以及顺式二氯二胺铂(II)的临床应用。作为唯一的化疗药物,该药物已被证明对多种小鼠肿瘤非常有效,并已成功与其他抗肿瘤药物如环磷酰胺和阿拉伯糖胞嘧啶联合使用。不幸的是,顺式二氯二胺铂(II)的治疗指数较低,肾脏毒性是其使用的主要限制。这促使了许多相关铂化合物的合成和测试,其中顺式二氯双环戊胺铂(II)和“铂蓝”似乎最有希望。在这些产品的合成、纯化和测试方面的经验将被讨论,并确定该领域尚未解决的突出问题。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Coordination complexes of platinum as antitumor agents.

Rosenberg and VanCamp first reported the bacteriostatic and antitumor properties of certain platinum coordination compounds. This pioneering work has led to the synthesis and testing of a large number of related platinum products and the clinical use of cis-dichlorodiammineplatinum (II). This drug has proven very efficacious against a wide variety of mouse tumors when employed as the sole chemotherapeutic agent and has also been combined successfully with other antitumor agents, such as cyclophosphamide and cytosine arabinsoide. Unfortunately, cis-dichlorodiammineplatinum (II) has a low therapeutic index with renal toxicity being the principal limitation of its use. This has prompted the synthesis and testing of many related platinum compounds, of which cis-dichlorobiscyclopentylamine-platinum (II) and the "platinum blues" appear most promising. Experience in the synthesis, purification, and testing of such products will be discussed together with identification of outstanding unsolved problems in this area.

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