Garuti Laura, Roberti Marinella, Pizzirani Daniela
Department of Pharmaceutical Science, University of Bologna, via Belmeloro 6, I-40126 Bologna, Italy.
Mini Rev Med Chem. 2007 May;7(5):481-9. doi: 10.2174/138955707780619626.
The development of prodrugs that are enzymatically activated into anticancer agents is a promising perspective in cancer therapy. Many nitrogen-containing quinoid heterocycles have been reported to show antitumor effect. The principal interest in these compounds lies on their potential to produce tumor-selective toxicity. Selectivity occurs by difference in oxygen tension between normal and tumor tissue and by levels of the required activating enzymes. In this review a summary of the most interesting heterocyclic quinones is given together with their biological property. SAR studies concerning the importance of some structural features will be described.
开发可通过酶促激活转化为抗癌剂的前药是癌症治疗中一个很有前景的方向。许多含氮醌类杂环化合物已被报道具有抗肿瘤作用。对这些化合物的主要兴趣在于它们产生肿瘤选择性毒性的潜力。选择性是通过正常组织和肿瘤组织之间的氧张力差异以及所需激活酶的水平来实现的。在这篇综述中，给出了最有趣的杂环醌类化合物及其生物学特性的总结。还将描述关于一些结构特征重要性的构效关系研究。
