Department of Medicinal Chemistry, Shantou University Medical College, Shantou, Guangdong 515041, P. R. China.
Dalton Trans. 2020 Dec 15;49(47):17173-17182. doi: 10.1039/d0dt02715d.
The osmium(vi) nitrido complex [OsVI(N)(sap)(py)Cl] is a potential anti-cancer drug with promising in vitro antiproliferative activities toward a panel of cancer cell lines, including cisplatin-resistant cells (IC50 values of 2.8-13.8 μM). This drug targets DNA and changes its conformation via covalent binding and insertion. In vitro studies indicate that the drug induces HepG2 cells G2/M phase arrest, disrupts the mitochondrial membrane potential and causes caspase-mediated apoptosis. Further in vivo studies using HepG2-bearing nude mice reveal that this drug not only shows good antitumor efficacy of inhibiting tumor growth, but also does not show the side effect of weight loss.
锇(VI)亚硝化物配合物[OsVI(N)(sap)(py)Cl]是一种有潜力的抗癌药物,对一系列癌细胞系具有良好的体外抗增殖活性,包括顺铂耐药细胞(IC50 值为 2.8-13.8 μM)。该药物靶向 DNA 并通过共价键结合和插入改变其构象。体外研究表明,该药物诱导 HepG2 细胞 G2/M 期阻滞,破坏线粒体膜电位并引发 caspase 介导的细胞凋亡。使用荷瘤裸鼠的进一步体内研究表明,该药物不仅表现出抑制肿瘤生长的良好抗肿瘤疗效,而且没有体重减轻的副作用。