Centro de Química Estrutural, Faculdade de Ciências da Universidade de Lisboa, Campo Grande, 1749-016, Lisbon, Portugal.
Centro de Química Estrutural, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, 1049-001, Lisbon, Portugal.
ChemMedChem. 2019 Apr 3;14(7):770-778. doi: 10.1002/cmdc.201800702. Epub 2019 Feb 20.
New cyclam derivatives (HOCH CH CH ) (PhCH ) Cyclam and (HOCH CH CH ) ( PhCH ) Cyclam, as well as their Cu and Fe complexes, were synthesized and characterized and their stability in cellular media was assessed. The cytotoxic effect of all compounds was examined on human cervical cancer (HeLa) cells, revealing strong anticancer activity. After 24 h, only complexes with the (HOCH CH CH ) ( PhCH ) Cyclam ligand are cytotoxic, whereas after incubation for 72 h all compounds show significant antiproliferative effects. Notably, compounds containing PhCH pendant arms on the cyclam ring revealed the most activity, with cytotoxicity values up to 12 times higher than those of cisplatin. All metal complexes seem to induce cell death through the formation of reactive oxygen species.
新的环脒衍生物（HOCHCHCH）（PhCH）环脒和（HOCHCHCH）（PhCH）环脒及其 Cu 和 Fe 配合物被合成并进行了表征，并评估了它们在细胞培养基中的稳定性。所有化合物的细胞毒性作用均在人宫颈癌（HeLa）细胞上进行了检查，结果显示出很强的抗癌活性。24 h 后，只有具有（HOCHCHCH）（PhCH）环脒配体的配合物具有细胞毒性，而在孵育 72 h 后，所有化合物均显示出明显的抗增殖作用。值得注意的是，环脒环上含有 PhCH 侧臂的化合物表现出最高的活性，其细胞毒性值比顺铂高 12 倍。所有金属配合物似乎都通过形成活性氧物种诱导细胞死亡。
