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生物还原药物的实验进展及其在癌症治疗中的作用。

The experimental development of bioreductive drugs and their role in cancer therapy.

作者信息

Workman P, Stratford I J

机构信息

Cancer Research Campaign Beatson Laboratories, CRC Department of Medical Oncology, University of Glasgow, Bearsden, United Kingdom.

出版信息

Cancer Metastasis Rev. 1993 Jun;12(2):73-82. doi: 10.1007/BF00689802.

Abstract

Bioreductive drugs undergo metabolic reduction to generate cytotoxic metabolites. This process is facilitated by bioreductive enzymes and the lower oxygen conditions present in solid tumours compared to normal tissues. Because of this specificity, bioreductive drugs have enormous potential to contribute to modern cancer therapy. Examples undergoing clinical trials include N-oxides such as tirapazamine, aziridinylnitroimidazoles RSU 1069/RBU 6145 and quinones such as indoloquinone EO9. Other novel structures are also under study. Here we review the experimental development of bioreductive drugs and their role in cancer therapy.

摘要

生物还原药物通过代谢还原产生细胞毒性代谢物。与正常组织相比,实体瘤中存在的生物还原酶和较低的氧含量促进了这一过程。由于这种特异性,生物还原药物在现代癌症治疗中具有巨大的贡献潜力。正在进行临床试验的例子包括N-氧化物如替拉扎明、氮丙啶基硝基咪唑RSU 1069/RBU 6145以及醌类如吲哚醌EO9。其他新型结构也在研究中。在此,我们综述生物还原药物的实验进展及其在癌症治疗中的作用。

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