Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi 221 005, U.P., India.
Centre for Genetic Disorders, Banaras Hindu University, Varanasi 221 005, U.P., India.
Dalton Trans. 2016 Apr 28;45(16):7163-77. doi: 10.1039/c6dt00446f.
Four organometallic complexes [(η(6)-C6H6)RuCl(pmpzdpm)], 1; [(η(6)-C6H6)RuCl(pypzdpm)], 2; [(η(6)-C10H14)RuCl(pmpzdpm)], 3 and [(η(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, (1)H, (13)C 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 μM,4 ).
四个有机金属配合物[(η(6)-C6H6)RuCl(pmpzdpm)]，1；[(η(6)-C6H6)RuCl(pypzdpm)]，2；[(η(6)-C10H14)RuCl(pmpzdpm)]，3 和 [(η(6)-C10H14)RuCl(pypzdpm)]，4，其中含有 5-(2-嘧啶基-哌嗪基)苯二吡咯甲川(pmpzdpm)和 5-(2-吡啶基哌嗪基)苯二吡咯甲川(pypzdpm)，已经被设计和合成。配合物 1-4 通过元素分析和光谱研究（ESI-MS、IR、(1)H、(13)C NMR、UV-vis）进行了全面表征。它们与 CT-DNA 的静电/嵌入相互作用通过 UV-vis 和竞争性溴化乙锭置换研究进行了研究，而它们与牛血清白蛋白（BSA）的蛋白质结合亲和力则通过 UV-vis、荧光、同步和三维（3D）荧光研究来实现。通过计算机模拟研究进一步验证了与 DNA 和蛋白质的相互作用。细胞摄取、体外细胞毒性和流式细胞术分析已用于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，这些配合物导致细胞周期在 subG1 期停滞，总体结果表明，1-4 的体外抗肿瘤活性顺序为 3>4>1>2（IC50，7.0μM）。
