Using a multigram-scalable synthesis, we obtained nine dinuclear complexes based on nonendogenous iron(I) centers and featuring variable aminocarbyne and P-ligands. One compound from the series (FEACYP) emerged for its strong cytotoxicity in vitro against four human cancer cell lines, surpassing the activity of cisplatin by 3–6 times in three cell lines, with an average selectivity index of 6.2 compared to noncancerous HEK293 cells. FEACYP demonstrated outstanding water solubility (15 g/L) and stability in physiological-like solutions. It confirmed its superior antiproliferative activity when tested in 3D spheroids of human pancreatic cancer cells and showed a capacity to inhibit thioredoxin reductase (TrxR) similar to auranofin. In vivo treatment of murine LLC carcinoma with FEACYP (8 mg kg^–1 dose) led to excellent tumor growth suppression (88%) on day 15, with no signs of systemic toxicity and only limited body weight loss.

中文翻译：

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1,3,5-Triaza-7-phosphaadamantane 和环己基赋予二铁 (I) 络合物水溶性和稳定性，并在细胞和动物模型中具有显着的抗癌活性


通过多克级规模的合成，我们获得了九种基于非内源性铁 (I) 中心并具有可变氨基卡宾和 P-配体的双核配合物。该系列中的一种化合物 (FEACYP) 因其在体外针对四种人类癌细胞系的强大细胞毒性而出现，在三种细胞系中的活性超过顺铂 3-6 倍，与非癌性 HEK293 细胞相比，平均选择性指数为 6.2。 FEACYP 在类似生理的溶液中表现出出色的水溶性 (15 g/L) 和稳定性。在人胰腺癌细胞的 3D 球体中进行测试时，证实了其卓越的抗增殖活性，并显示出与金诺芬类似的抑制硫氧还蛋白还原酶 (TrxR) 的能力。用 FEACYP（8 mg kg ^–1 剂量）对小鼠 LLC 癌进行体内治疗，第 15 天可实现出色的肿瘤生长抑制（88%），没有全身毒性迹象，体重减轻有限。