金（III）基化合物在生理环境中的化学稳定性有限，这一点一直是药物研发中的挑战，有机金属化学可能提供解决这个问题的方法。本文介绍了四种新型阳离子有机金（III）-硫代氨基甲酸盐配合物的一般结构[(C^N)AuIIIDTC]PF6（C1a-C4a，DTC=硫代氨基甲酸盐，L1-L4，C^N=2-苯胺基吡啶），并将其与其配位金（III）-硫代氨基甲酸盐类似物[AuIIIDTCCl2]（C1b-C4b）进行了比较，作为潜在的抗癌和抗利什曼病药物。大多数配合物有效抑制肿瘤细胞的生长，特别是C3a对乳腺癌（MCF-7和MDA-MB-231细胞）表现出纳摩尔范围内的抗增殖效应，并具有适度的选择性。对C3a处理后的MCF-7细胞进行的促凋亡研究显示，早期凋亡细胞的数量很高。C3a与模型巯基（N-乙酰-L-半胱氨酸）的反应性研究提示可能涉及有机金（III）-核心与巯酸盐之间的结合作用。在忽视的疾病范围内，金配合物作为利什曼病的有前途的治疗替代方法正在兴起。在这方面，所有金（III）-硫代氨基甲酸盐配合物对至少一种利什曼病菌株表现出抗利什曼病活性。C1a、C4a、C1b、C4b对所有测试的寄生虫均表现出IC50值在0.12至42 μM之间变化的活性，而总体上，有机金属化合物显示出更有趣的抑制特性。C4a对L. braziliensis的选择性高于500倍，甚至高于参考的抗利什曼病药物两性霉素B。总的来说，我们的研究结果表明，有机金（III）基团在抗癌和抗利什曼病效果上显著增强，相比配位类似物；因此，显示出有机金属化学在基于金属药物的癌症和利什曼病化疗中的巨大潜力。Copyright © 2023 Elsevier Inc. All rights reserved.

The limited chemical stability of gold(III)-based compounds in physiological environment has been a challenge in drug discovery, and organometallic chemistry might provide the solution to overcome this issue. In this work, four novel cationic organogold(III)-dithiocarbamate complexes of general structure [(C^N)AuIIIDTC]PF6 (C1a - C4a, DTC = dithiocarbamate, L1 - L4, C^N = 2-anilinopyridine) are presented, and compared to their coordination gold(III)-dithiocarbamate analogues [AuIIIDTCCl2] (C1b - C4b), as potential anti-cancer and anti-leishmanial drugs. Most of the complexes effectively inhibited cancer cell growth, notably C3a presented anti-proliferative effect in the nanomolar range against breast cancer (MCF-7 and MDA-MB-231 cells with moderate selectivity. Pro-apoptotic studies on treated MCF-7 cells showed a high population of cells in early apoptosis. Reactivity studies of C3a towards model thiols (N-acetyl-L-cysteine) refer to a possible mode of action involving bonding between the organogold(III)-core and the thiolate. In the scope of neglected diseases, gold complexes are emerging as promising therapeutic alternatives against leishmaniasis. In this regard, all gold(III)-dithiocarbamate complexes presented anti-leishmanial activity against at least one Leishmania species. Complexes C1a, C4a, C1b, C4b were active against all tested parasites with IC50 values varying between 0.12 and 42 μM, and, overall, organometallic compounds presented more intriguing inhibition profiles. For C4a selectivity over 500-fold for L. braziliensis; even higher than the reference anti-leishmanial drug amphotericin B. Overall, our findings revealed that the organogold(III) moiety significantly amplified the anti-cancer and anti-leishmanial effects with respect to the coordination analogues; thus, showing the great potential of organometallic chemistry in metallodrug-based chemotherapy for cancer and leishmaniasis.Copyright © 2023 Elsevier Inc. All rights reserved.