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[Ru(phen)2podppz]2+ significantly inhibits glioblastoma growth in vitro and vivo with fewer side-effects than cisplatin.
Dalton Transactions ( IF 3.5 ) Pub Date : 2020-06-16 , DOI: 10.1039/d0dt01877e Ruihao Li 1 , Yabin Ma , Xiaochun Hu , Wenjing Wu , Xuewen Wu , Chunyan Dong , Shuo Shi , Yun Lin
Dalton Transactions ( IF 3.5 ) Pub Date : 2020-06-16 , DOI: 10.1039/d0dt01877e Ruihao Li 1 , Yabin Ma , Xiaochun Hu , Wenjing Wu , Xuewen Wu , Chunyan Dong , Shuo Shi , Yun Lin
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To overcome the acquired resistance and the significant side-effects of the reported drugs, four new ruthenium(II) complexes with alkynyl (Ru1, Ru2, Ru3, Ru4) were designed and synthesized. Ru1, Ru2, Ru3 and Ru4 were characterized by ESI-MS, 1H NMR, 1H–1H COSY NMR and elemental analysis. Compared with Ru2, Ru3, Ru4 and cisplatin, the anti-tumor experiments in vitro and vivo confirmed that Ru1 could most effectively inhibit tumor growth. In the experiments of safety evaluation in vivo, Ru1 could avoid any detectable side-effects compared with cisplatin. DNA binding experiments and cell cycle experiments showed that Ru1 exhibited the strongest DNA binding ability and interfered with the cell cycle by inserting DNA to inhibit tumor growth. The study demonstrated that Ru1 had the potential to be an exciting new drug candidate for glioblastoma treatment.
中文翻译：
[Ru（phen）2podppz] 2+在体外和体内均显着抑制胶质母细胞瘤的生长，且副作用少于顺铂。
为了克服所报道药物的获得性耐药性和明显的副作用，设计并合成了四种新的具有炔基的钌（II）配合物（Ru1，Ru2，Ru3，Ru4）。通过ESI-MS，1 H NMR，1 H– 1 H COZY NMR和元素分析对Ru1，Ru2，Ru3和Ru4进行表征。与Ru2，Ru3，Ru4和顺铂相比，体外和体内抗肿瘤实验证实：Ru1可以最有效地抑制肿瘤的生长。在体内安全性评估实验中，Ru1与顺铂相比可避免任何可检测到的副作用。DNA结合实验和细胞周期实验表明，Ru1表现出最强的DNA结合能力，并通过插入DNA抑制肿瘤生长来干扰细胞周期。该研究表明Ru1有潜力成为治疗胶质母细胞瘤的激动人心的新药。
更新日期：2020-07-07
中文翻译：
[Ru（phen）2podppz] 2+在体外和体内均显着抑制胶质母细胞瘤的生长，且副作用少于顺铂。
为了克服所报道药物的获得性耐药性和明显的副作用，设计并合成了四种新的具有炔基的钌（II）配合物（Ru1，Ru2，Ru3，Ru4）。通过ESI-MS，1 H NMR，1 H– 1 H COZY NMR和元素分析对Ru1，Ru2，Ru3和Ru4进行表征。与Ru2，Ru3，Ru4和顺铂相比，体外和体内抗肿瘤实验证实：Ru1可以最有效地抑制肿瘤的生长。在体内安全性评估实验中，Ru1与顺铂相比可避免任何可检测到的副作用。DNA结合实验和细胞周期实验表明，Ru1表现出最强的DNA结合能力，并通过插入DNA抑制肿瘤生长来干扰细胞周期。该研究表明Ru1有潜力成为治疗胶质母细胞瘤的激动人心的新药。
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