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Pharmacological applications of non-radioactive indium(III) complexes: A field yet to be explored
Coordination Chemistry Reviews ( IF 20.6 ) Pub Date : 2020-05-26 , DOI: 10.1016/j.ccr.2020.213375
Heloisa Beraldo

Although radioactive 111In(III) compounds have been extensively investigated for labeling of cells in detection and diagnosis of infections and inflammation, the pharmacological applications of non-radioactive indium(III) complexes remain so far almost unexplored. In the present work the main potential applications of these complexes as antimicrobial and antineoplastic agents are reviewed, together with their interactions with different biomolecules. Some aspects of the behavior of indium(III) complexes in biological aqueous media are also mentioned. The interactions of indium(III) complexes with transferrin are discussed, with emphasis in the potential applications of these compounds for the treatment of tumors which overexpress transferrin receptors. Hence, the affinity of indium(III) complexes for transferrin might be explored in the design of selective antineoplastic agents. Some preliminary information on the toxicity of these complexes is given as well, which must be taken into consideration in evaluating the efficacy, safety and druggability of indium(III) complexes. Since 111In compounds are already used in clinics, non-radioactive indium(III) complexes might be an attractive platform for developing novel metal-based antitumor drug candidates.



中文翻译:

非放射性铟(III)配合物的药理应用:尚未探索的领域

虽然放射性111In(III)化合物已被广泛研究以标记细胞以检测和诊断感染和炎症,到目前为止,非放射性In(III)络合物的药理应用仍未开发。在目前的工作中,这些复合物作为抗微生物和抗肿瘤药的主要潜在应用,以及它们与不同生物分子的相互作用,都进行了综述。还提到了铟(III)配合物在生物水性介质中行为的某些方面。讨论了铟(III)配合物与运铁蛋白的相互作用,重点是这些化合物在治疗过表达运铁蛋白受体的肿瘤中的潜在应用。因此,铟(III)配合物对转铁蛋白的亲和力可在选择性抗肿瘤药的设计中探索。还给出了有关这些配合物毒性的一些初步信息,在评估铟(III)配合物的功效,安全性和可药用性时必须考虑这些信息。以来111在已经用于临床的化合物中,非放射性铟(III)配合物可能是开发新型基于金属的抗肿瘤药物候选物的有吸引力的平台。

更新日期:2020-05-26
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