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诺加霉素及其衍生物的生化药理学

The biochemical pharmacology of nogalamycin and its derivatives.

作者信息

Li L H, Krueger W C

机构信息

Upjohn Laboratories, Upjohn Company, Kalamazoo, MI 49001.

出版信息

Pharmacol Ther. 1991;51(2):239-55. doi: 10.1016/0163-7258(91)90080-6.

Abstract

This review assimilates up-to-date information on the biochemical pharmacology of nogalamycin and selected derivatives that have shown good biological activities and/or received a relatively detailed investigation. The structure and chemical preparation of these derivatives from nogalamycin is described and the nomenclature which has been rather perplexing in the literature is clarified. The interaction of this class of compounds, particularly nogalamycin, with DNA is extensively reviewed. The biochemical mechanism of action of nogalamycin and its structurally closely-related derivatives is described. Among nogalamycin derivatives, menogaril showed distinct biochemical effects as well as superior cytotoxicity and antitumor activity and also proved to be effective against breast cancer clinically.

摘要

本综述汇总了关于诺加霉素及其选定衍生物的生化药理学的最新信息,这些衍生物已显示出良好的生物活性和/或受到了较为详细的研究。描述了这些诺加霉素衍生物的结构和化学制备方法,并澄清了文献中一直相当令人困惑的命名法。广泛综述了这类化合物,特别是诺加霉素与DNA的相互作用。描述了诺加霉素及其结构密切相关的衍生物的生化作用机制。在诺加霉素衍生物中,美诺加明表现出独特的生化效应以及卓越的细胞毒性和抗肿瘤活性,并且在临床上也被证明对乳腺癌有效。

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