Heteroleptic arene Ru(II) dipyrrinato complexes: DNA, protein binding and anti-cancer activity against the ACHN cancer cell line

Gupta Rakesh Kumar; Kumar Amit; Paitandi Rajendra Prasad; Singh Roop Shikha; Mukhopadhyay Sujay; Verma Shiv Prakash; Das Parimal; Pandey Daya Shankar

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Heteroleptic arene Ru(II) dipyrrinato complexes: DNA, protein binding and anti-cancer activity against the ACHN cancer cell line

机译：异戊二烯Ru（II）dipyrrinato复合物：DNA，蛋白质结合和针对ACHN癌细胞系的抗癌活性

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Four organometallic complexes [(eta(6)-C6H6) RuCl(pmpzdpm)], 1; [(eta(6)-C6H6) RuCl(pypzdpm)], 2; [(eta(6)-C10H14) RuCl(pmpzdpm)], 3 and [(eta(6)-C10H14) RuCl(pypzdpm)], 4 containing 5-(2-pyrimidyl-piperazine) phenyldipyrromethene (pmpzdpm) and 5-(2-pyridylpiperazine) phenyldipyrromethene (pypzdpm) have been designed and synthesized. The complexes 1-4 have been fully characterized by elemental analyses and spectroscopic studies (ESI-MS, IR, H-1, C-13 NMR, UV-vis). Their electrostatic/intercalative interaction with CT DNA has been investigated by UV-vis and competitive ethidium bromide displacement studies while their protein binding affinity toward bovine serum albumin (BSA) was realized by UV-vis, fluorescence, synchronous and three dimensional (3D) fluorescence studies. The interaction with DNA and protein has further been validated by in silico studies. Cellular uptake, in vitro cytotoxicity and flow cytometric analyses have been performed to determine the mode of cell death against the kidney cancer cell line ACHN. Cell cycle analysis suggested that the complexes cause cell cycle arrest in the subG1 phase and overall results indicated that the in vitro antitumor activity of 1-4 lies in the order of 3 > 4 > 1 > 2 (IC50, 7.0 1; 8.0 2; 2.0 3; 4.0 mu M, 4).

机译：四种有机金属配合物[（eta（6）-C6H6）RuCl（pmpzdpm）]，1; [（eta（6）-C6H6）RuCl（pypzdpm）]，2; [（eta（6）-C10H14）RuCl（pmpzdpm）]，3和[[eta（6）-C10H14）RuCl（pypzdpm）]，4，含有5-（2-嘧啶基-哌嗪）苯基二吡咯亚甲基（pmpzdpm）和5-已经设计并合成了（2-吡啶基哌嗪）苯基二吡咯亚甲基（pypzdpm）。配合物1-4已通过元素分析和光谱研究（ESI-MS，IR，H-1，C-13 NMR，UV-vis）充分表征。通过紫外可见和竞争性溴化乙锭置换研究了它们与CT DNA的静电/插入相互作用，同时通过紫外可见，荧光，同步和三维（3D）荧光实现了它们对牛血清白蛋白（BSA）的蛋白结合亲和力。学习。通过计算机研究进一步证实了与DNA和蛋白质的相互作用。已经进行了细胞摄取，体外细胞毒性和流式细胞术分析以确定针对肾癌细胞系ACHN的细胞死亡模式。细胞周期分析表明，该复合物导致subG1期细胞周期停滞，总体结果表明，体外抗肿瘤活性1-4的顺序为3> 4> 1> 2（IC50，7.0 1; 8.0 2; 2.0 3; 4.0μM，4）。

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《Dalton transactions: An international journal of inorganic chemistry》 |2016年第16期|共15页
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Gupta Rakesh Kumar; Kumar Amit; Paitandi Rajendra Prasad; Singh Roop Shikha; Mukhopadhyay Sujay; Verma Shiv Prakash; Das Parimal; Pandey Daya Shankar;
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1. Heteroleptic arene Ru(II) dipyrrinato complexes: DNA, protein binding and anti-cancer activity against the ACHN cancer cell line [J] . Gupta Rakesh Kumar, Kumar Amit, Paitandi Rajendra Prasad, Dalton transactions: An international journal of inorganic chemistry . 2016,第16期

机译：异戊二烯Ru（II）dipyrrinato复合物：DNA，蛋白质结合和针对ACHN癌细胞系的抗癌活性
2. Interaction of ferrocene appended Ru(II), Rh(III) and Ir(III) dipyrrinato complexes with DNA/protein, molecular docking and antitumor activity [J] . Paitandi Rajendra Prasad, Gupta Rakesh Kumar, Singh Roop Shikha, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2014,第期

机译：与DNA /蛋白，分子对接和抗肿瘤活性的二茂铁（II），RH（III），RH（III），RH（III）和IR（III）二吡啶复合物的相互作用
3. Effect of ligand substitution in pyrazolone based binary and ternary Cu(II) complexes on DNA binding, protein binding and anti-cancer activity on A549 lung carcinoma cell lines [J] . Komal M. Vyas, R.N. Jadeja, Dipak Patel, Polyhedron: The International Journal for Inorganic and Organometallic Chemistry . 2014,第Null期

机译：吡唑啉酮二元和三元Cu（II）配合物中配体取代对A549肺癌细胞系DNA结合，蛋白质结合和抗癌活性的影响
4. Towards an understanding of protein-protein interaction network hierarchies. Analysis of DnaN (β)-binding peptide motifs in members of protein families interacting with the eubacterial processivity clamp, the β subunit of DNA Polymerase III [C] . Brian P. Dalrymple, Gene Wijffels, Kritaya Kongsuwan, Asia-Pacific Bioinformatics Conference(APBC 2003); 200302; Adelaide(AU) . 2003

机译：对蛋白质-蛋白质相互作用网络层次结构的理解。蛋白质家族成员与DNA聚合酶III的优生过程性钳位相互作用的DnaN（β）结合肽基序分析
5. The structure and reactivity of a series of high-valent oxo complexes of Ru and Mn: Ru(III)-mediated catalytic oxygenation of triphenylphosphine, characterization of binuclear Mn(III,III) and Mn(III,IV) dimers, and mononuclear iron(III) and iron(IV). [D] . Fackler, Nathanael L. P. 1997

机译：Ru和Mn的一系列高价羰基配合物的结构和反应性：Ru（III）介导的三苯膦催化氧化，双核Mn（III，III）和Mn（III，IV）二聚体的表征以及单核铁（III）和铁（IV）。
6. Design Synthesis DNA/HSA Binding and CytotoxicActivity of Half-Sandwich Ru(II)-Arene Complexes Containing Triarylamine–ThiosemicarbazoneHybrids [O] . Mathiyan Muralisankar, Ramachandran Dheepika, Jebiti Haribabu, 2019

机译：设计合成DNA / HSA结合和细胞毒性含三芳基胺-硫代氨基脲的半三明治Ru（II）-芳烃配合物的活性杂种
7. Conformation of DNA Modified by Monofunctional Ru(II) Arene Complexes: Recognition by DNA Binding Proteins and Repair. Relationship to Cytotoxicity [O] . Novakova Olga, Kasparkova Jana, Bursova Vendula, 2005

机译：由单官能Ru（II）芳烃配合物修饰的DNA的构象：DNA结合蛋白的识别和修复。与细胞毒性的关系

Heteroleptic arene Ru(II) dipyrrinato complexes: DNA, protein binding and anti-cancer activity against the ACHN cancer cell line

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