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铑配合物生物活性的最新进展:在药物发现研究中的应用。

Recent advances in biological activities of rhodium complexes: Their applications in drug discovery research.

机构信息

Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran.

Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran; Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

Eur J Med Chem. 2021 Apr 15;216:113308. doi: 10.1016/j.ejmech.2021.113308. Epub 2021 Feb 23.

DOI:10.1016/j.ejmech.2021.113308
PMID:33713976
Abstract

Unique structure, characteristic reactivity, and facile synthesis of metal complexes have made them efficient ligands in drug development research. Among them, rhodium complexes have a limited history and there are a few discussions about their biological activities documented in the literature. However, investigation of kinetically inert rhodium complexes has recently attracted lots of attention and especially there are various evidences on their anti-cancer activity. It seems that they can be investigated as a versatile surrogates or candidates for the existing drugs which do not affect selectively or suffer from various side effects. In recent years, there has been an increasing interest in the use of mononuclear rhodium (III) organometallo drugs due to its versatile structurally important aspects to inhibit various enzymes. It has been demonstrated that organometallic Rh complexes profiting from both organic and inorganic aspects have shown more potent biological activities than classical inorganic compartments. In this respect, smart design, use of the appropriate organic ligands, and efficient and user-friendly synthesis of organometallic Rh complexes have played crucial roles in the inducing desirable biological activities. In this review, we focused on the recent advances published on the bioactivity of Rh (III/II/I) complexes especially inhibitory activity, from 2013 till now. Accordingly, considering the structure-activity relationship (SAR), the effect of oxidation state (+1, +2, and +3) and geometry (dimer or monomer complexes with coordination number of 4 and 6) of Rh complexes as well as various ligands on in vitro and in vivo studies was comprehensively discussed.

摘要

金属配合物具有独特的结构、特征反应性和易于合成的特点,因此它们是药物开发研究中有效的配体。其中,铑配合物的历史有限,文献中仅有一些关于其生物活性的讨论。然而,最近人们对动力学惰性铑配合物的研究产生了浓厚的兴趣,特别是有大量证据表明它们具有抗癌活性。它们似乎可以作为现有药物的多功能替代品或候选物进行研究,这些药物不会选择性地影响或受到各种副作用的影响。近年来,由于单核铑(III)有机金属药物在抑制各种酶方面具有多种多样的结构重要方面,因此人们对其的使用越来越感兴趣。已经证明,从有机和无机两方面受益的有机金属 Rh 配合物比经典的无机化合物具有更强的生物活性。在这方面,智能设计、使用适当的有机配体以及高效、用户友好的有机金属 Rh 配合物的合成在诱导所需的生物活性方面发挥了至关重要的作用。在这篇综述中,我们重点介绍了 2013 年至今发表的有关 Rh(III/II/I)配合物生物活性的最新进展,特别是抑制活性。因此,考虑到结构-活性关系(SAR)、氧化态(+1、+2 和+3)和几何形状(具有 4 和 6 配位数的二聚体或单体配合物)以及各种配体对体外和体内研究的影响,我们对其进行了全面讨论。

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