Nardon Chiara, Fregona Dolores
Department of Chemical Sciences University of Padua, via Marzolo 1, 35131 Padova, Italy.
Curr Top Med Chem. 2016;16(3):360-80. doi: 10.2174/1568026615666150827094500.
In the last decade, we have been developing some gold(III) derivatives showing interesting antitumor properties and reduced systemic and renal toxicity, compared to the clinically-established reference drug cisplatin. Starting from the rationale at the base of our investigations, this review has been divided into two sections, with respect to our patented first- (aminoderivatives) and secondgeneration (peptidomimetics) potential drugs. Every section describes the in vitro and in vivo anticancer activity of the compounds, chosen as models, towards different types of tumor. In particular, we summarize the results achieved so far, in particular taking into account the latest in-depth studies related to their activity, mechanism of action and toxicological profile. Taken together, our data could open up new prospects for further advanced preclinical pharmacological testing.
在过去十年中，我们一直在研发一些金（III）衍生物，与临床常用的参考药物顺铂相比，这些衍生物显示出有趣的抗肿瘤特性，且全身毒性和肾毒性降低。基于我们研究的基本原理，本综述分为两个部分，分别介绍我们获得专利的第一代（氨基衍生物）和第二代（肽模拟物）潜在药物。每个部分都描述了作为模型的化合物对不同类型肿瘤的体外和体内抗癌活性。特别是，我们总结了迄今为止取得的成果，尤其考虑到了与其活性、作用机制和毒理学概况相关的最新深入研究。综合来看，我们的数据可能为进一步的临床前药理测试开辟新的前景。
