摘要
黄金在人类的历史上总会引起人们极大的兴趣。数千年中它被用于的珠宝,宗教信仰的贵重物品,耐用物品和艺术界。然而,很少有人知道,这样一种珍贵的金属在过去也被古人以其治疗性能加以利用。如今在二十世纪,一些含有氧化态+1金核的复合物被用来进行治疗类风湿性关节炎的研究,并且口服药物金诺芬也在1985被FDA批准上市。从化学的角度来看,黄金衍生物应值得特别关注,因为这种金属在元素周期表中处于特殊的位置,这就导致其不同寻常的相对特性,在所有金属中具有最高的电负性,电子亲和力和氧化还原能力。 本文在介绍了黄金复合物在医学中的使用之后,我们查阅了所有国际上或本国内在2010-2015年(直到2015年12月31日)发表的描述新的含有金(I)和金(III)无机化合物且已证实具有治疗特性的相关专利。这些专利主要是用以保护一些具有良好的抗癌(18个)和抗炎活性(4个)的化合物的利益。特别指出的是,这项工作探究了含有不同配位原子(如N、O、S、P)的配位化合物以及至少具有一个Au-C键的有机黄金衍生物。我们对一些报道了黄金衍生物毒性特点和细胞内的靶位点的专利也进行了讨论。
关键词: Auranofin
Current Medicinal Chemistry
Title:Gold Complexes for Therapeutic Purposes: an Updated Patent Review (2010-2015)
Volume: 23 Issue: 29
Author(s): Chiara Nardon, Nicolò Pettenuzzo, Dolores Fregona
Affiliation:
关键词: Auranofin
摘要: Gold has always aroused great interest in the history of mankind. It has been used for thousands of years for jewelry, religious cult valuables, durable goods and in the art world. However, few know that such a precious and noble metal was exploited in the past by the ancients also for its therapeutic properties. More recently, in the twentieth century some complexes containing gold centers in the oxidation state +1 were studied for the treatment of the rheumatoid arthritis and the orally-administered drug Auranofin was approved by the FDA in 1985. From the chemical point of view, gold derivatives deserve special attention due to the unique position of this metal within the periodic table, which results in unconventional relativistic effects and, ultimately, in the highest electronegativity, electron affinity and redox potential among all metals.
In this review, after an introduction concerning the use of gold complexes in medicine, we have examined all the patents internationally or nationally published in the years 2010-2015 (until December 31, 2015) and describing new inorganic compounds containing gold(I) and gold(III) with proved therapeutic properties. These patents were filed to mainly protect compounds with promising anticancer and anti-inflammatory activities (total 18 and 4, respectively). In particular, this work explores both coordination compounds containing ligands with various donor atoms (e.g., N-, O-, S- and -P) and organo-gold derivatives with at least one Au-C bond. The toxicological profile and the intracellular targets reported for some among the patented gold derivatives are discussed.
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Chiara Nardon, Nicolò Pettenuzzo, Dolores Fregona , Gold Complexes for Therapeutic Purposes: an Updated Patent Review (2010-2015), Current Medicinal Chemistry 2016; 23 (29) . https://dx.doi.org/10.2174/0929867323666160504103843
DOI https://dx.doi.org/10.2174/0929867323666160504103843 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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