Synthesis, structures, cellular uptake and apoptosis-inducing properties of highly cytotoxic ruthenium-Norharman complexes

Tan C.; Wu S.; Lai S.; Wang M.; Chen Y.; Zhou L.; Zhu Y.; Lian W.; Peng W.; Ji L.; Xu A.

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Synthesis, structures, cellular uptake and apoptosis-inducing properties of highly cytotoxic ruthenium-Norharman complexes

机译：高度细胞毒性钌-诺曼曼复合物的合成，结构，细胞摄取和凋亡诱导特性

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Three novel Ru(ii) complexes of the general formula [Ru(N-N) _2(Norharman)_2](SO_3CF_3)_2, where N-N = 2,2′-bipyridine (bpy, 1), 1,10-phenanthroline (phen, 2), 4,7-diphenyl-1,10-phenanthroline (DIP, 3) and Norharman (9H-pyrido[3,4-b]indole) is a naturally occurring β-carboline alkaloid, have been synthesized and characterized. The molecular structures of 1 and 2 have been determined by X-ray diffraction analysis. The cellular uptake efficiencies, in vitro cytotoxicities and apoptosis-inducing properties of these complexes have been extensively explored. Notably, 1-3 exhibit potent antiproliferative activities against a panel of human cancer cell lines with IC_(50) values lower than those of cisplatin. Further studies show that 1-3 can cause cell cycle arrest in the G0/G1 phase and induce apoptosis through mitochondrial dysfunction and reactive oxygen species (ROS) generation. In vitro DNA binding studies have also been conducted to provide information about the possible mechanism of action.

机译：三种通式为[Ru（NN）_2（Norharman）_2]（SO_3CF_3）_2的新型Ru（ii）络合物，其中NN = 2,2'-联吡啶（bpy，1），1,10-菲咯啉（phen， 2），已合成并表征了4,7-二苯基-1,10-菲咯啉（DIP，3）和Norharman（9H-吡啶并[3,4-b]吲哚）是天然存在的β-咔啉生物碱。 1和2的分子结构已经通过X射线衍射分析确定。这些复合物的细胞摄取效率，体外细胞毒性和细胞凋亡诱导特性已得到广泛研究。值得注意的是，1-3表现出对一组人类癌细胞的有效抗增殖活性，其IC_（50）值低于顺铂。进一步的研究表明，1-3可以导致细胞周期停滞在G0 / G1期，并通过线粒体功能障碍和活性氧（ROS）生成诱导凋亡。还进行了体外DNA结合研究，以提供有关可能的作用机制的信息。

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《Dalton transactions: An international journal of inorganic chemistry》 |2011年第34期|共11页
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Tan C.; Wu S.; Lai S.; Wang M.; Chen Y.; Zhou L.; Zhu Y.; Lian W.; Peng W.; Ji L.; Xu A.;
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1. Synthesis, structures, cellular uptake and apoptosis-inducing properties of highly cytotoxic ruthenium-Norharman complexes [J] . Tan C., Wu S., Lai S., Dalton transactions: An international journal of inorganic chemistry . 2011,第34期

机译：高度细胞毒性钌-诺曼曼复合物的合成，结构，细胞摄取和凋亡诱导特性
2. A comparative study on in vitro cytotoxicity, cellular uptake, localization and apoptosis-inducing mechanism of two ruthenium(II) complexes [J] . Chen Jincan, Zhang Yao, Li Baojun, Transition Metal Chemistry . 2018,第2期

机译：两种钌（II）复合物的体外细胞毒性，细胞吸收，定位和凋亡诱导机理的比较研究
3. New palladium(II) and platinum(II) 5,5-diethylbarbiturate complexes with 2-phenylpyridine, 2,2 '-bipyridine and 2,2 '-dipyridylamine: synthesis, structures, DNA binding, molecular docking, cellular uptake, antioxidant activity and cytotoxicity [J] . Icsel Ceyda, Yilmaz Veysel T., Kaya Yunus, Dalton transactions: An international journal of inorganic chemistry . 2015,第15期

机译：新的5,5-二乙基巴比妥酸钯（II）和铂（II）与2-苯基吡啶，2,2'-联吡啶和2,2'-二吡啶胺的络合物：合成，结构，DNA结合，分子对接，细胞吸收，抗氧化活性和细胞毒性
4. Novel highly symmetrical class of lanthanide tetrakis-complexes Na(H_2O)4LnL_4 (HL -l,3-bis(l,3-dimethyl-lH-pyrazol-4-yl)-l,3-propandione) - synthesis, crystal structure and unique photophysical properties. [C] . Ilva V. Tavdakov, Igor Ch. Avetisov, Konstantin A. Lyssenko Rare Earth Research Conference . 2019

机译：新型高度对称等级的镧系元素镧系元素Na（H_2O）4 LNL_4（HL_4（HL -L，3-双（L，3-二甲基-1H-吡唑-4-基）-L，3-PROPANCIONE） - 合成，晶体结构和独特的光药性。
5. Development of metal-metal quadruply bonded complexes with pi-extended structures: Synthesis, characterization, photophysical properties and applications as molecular synthons. [D] . Spilker, Thomas F. 2014

机译：具有π-延伸结构的金属-金属四重键合复合物的开发：合成，表征，光物理性质和作为分子合成子的应用。
6. Synthesis Characterization In Vitro Cytotoxicity and Apoptosis-Inducing Properties of Ruthenium(II) Complexes [O] . Li Xu, Nan-Jing Zhong, Yang-Yin Xie, -1

机译：钌（II）配合物的合成表征体外细胞毒性和细胞凋亡诱导特性
7. New palladium(II) and platinum(II) 5,5-diethylbarbiturate complexes with 2-phenylpyridine, 2,2’-bipyridine and 2,2’-dipyridylamine : synthesis, structures, DNA binding, molecular docking, cellular uptake, antioxidant activity and cytotoxicity [O] . Icsel, Ceyda, Yilmaz, Veysel T., Kaya, Yunus, 2015

机译：新的5,5-二乙基巴比妥酸钯（II）和铂（II）与2-苯基吡啶，2,2'-联吡啶和2,2'-二吡啶胺的络合物：合成，结构，DNA结合，分子对接，细胞吸收，抗氧化活性和细胞毒性

Synthesis, structures, cellular uptake and apoptosis-inducing properties of highly cytotoxic ruthenium-Norharman complexes

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