School of Chemistry, The University of Melbourne, Melbourne, 3010, Australia.
Chem Soc Rev. 2011 May;40(5):3005-18. doi: 10.1039/c0cs00215a. Epub 2011 Mar 15.
The molecules known as bis(thiosemicarbazones) derived from 1,2-diones can act as tetradentate ligands for Cu(II), forming stable, neutral complexes. As a family, these complexes possess fascinating biological activity. This critical review presents an historical perspective of their progression from potential chemotherapeutics through to more recent applications in nuclear medicine. Methods of synthesis are presented followed by studies focusing on their potential application as anti-cancer agents and more recent investigations into their potential as therapeutics for Alzheimer's disease. The Cu(II) complexes are of sufficient stability to be used to coordinate copper radioisotopes for application in diagnostic and therapeutic radiopharmaceuticals. Detailed understanding of the coordination chemistry has allowed careful manipulation of the metal based properties to engineer specific biological activities. Perhaps the most promising complex radiolabelled with copper radioisotopes to date is Cu(II)(atsm), which has progressed to clinical trials in humans (162 references).
双（硫代缩氨基甲肟）类化合物来源于 1,2-二酮，可以作为 Cu(II) 的四齿配体，形成稳定的中性配合物。作为一个家族，这些配合物具有迷人的生物活性。这篇评论从潜在的化疗药物的角度出发，介绍了它们的发展历程，以及最近在核医学中的应用。本文介绍了合成方法，并重点研究了它们作为抗癌药物的潜在应用，以及最近对其作为阿尔茨海默病治疗药物的研究。Cu(II) 配合物具有足够的稳定性，可用于与铜放射性同位素配位，应用于诊断和治疗放射性药物。对配位化学的深入了解允许对金属基特性进行精细操作，以设计特定的生物活性。到目前为止，用铜放射性同位素标记的最有前途的配合物是 Cu(II)(atsm)，它已经进入了人体临床试验（162 篇参考文献）。
