Department of Chemistry, Faculty of Science, Banaras Hindu University, Varanasi 221 005, U.P., India.
Department of Zoology, Faculty of Science, Banaras Hindu University, Varanasi 221 005, U.P., India.
Eur J Med Chem. 2014 Sep 12;84:17-29. doi: 10.1016/j.ejmech.2014.06.052. Epub 2014 Jun 26.
Efficacy of the ferrocene appended piano-stool dipyrrinato complexes [(η(6)-C6H6)RuCl(fcdpm)] (1), [(η(6)-C10H14)RuCl(fcdpm)] (2), [(η(6)-C12H18)RuCl(fcdpm)] (3) [(η(5)-C5Me5)RhCl(fcdpm)] (4) and [(η(5)-C5Me5)IrCl(fcdpm)] (5) [fcdpm = 5-ferrocenyldipyrromethene] toward anticancer activity have been described. Binding of the complexes with calf thymus DNA (CT-DNA) and BSA (bovine serum albumin) have been thoroughly investigated by UV-Vis and fluorescence spectroscopy. Binding constants for 1-5 (range, 10(4)-10(5) M(-1)) validated their efficient binding with CT-DNA. Molecular docking studies revealed interaction through minor groove of the DNA, on the other hand these also interact through hydrophobic residues of the protein, particularly cavity in the subdomain IIA. In vitro anticancer activity have been scrutinized by MTT assay, acridine orange/ethidium bromide (AO/EtBr) fluorescence staining, and DNA ladder (fragmentation) assay against Dalton's Lymphoma (DL) cells. Present study revealed that rhodium complex (4) is more effective relative to ruthenium (1-3) and iridium (5) complexes.
已经描述了 [(η(6)-C6H6)RuCl(fcdpm)] (1)、[(η(6)-C10H14)RuCl(fcdpm)] (2)、[(η(6)-C12H18)RuCl(fcdpm)] (3)、[(η(5)-C5Me5)RhCl(fcdpm)] (4) 和 [(η(5)-C5Me5)IrCl(fcdpm)] (5)（fcdpm = 5-二茂铁基二吡咯甲川）这些钌和铑 appended 钢琴凳二吡咯甲川配合物在抗癌活性方面的功效。通过紫外可见光谱和荧光光谱法深入研究了配合物与小牛胸腺 DNA（CT-DNA）和牛血清白蛋白（BSA）的结合。配合物 1-5（范围为 10(4)-10(5) M(-1)）的结合常数证明了它们与 CT-DNA 的有效结合。分子对接研究表明，这些配合物通过 DNA 的小沟相互作用，另一方面，它们也通过蛋白质的疏水性残基相互作用，特别是亚结构域 IIA 中的空腔。通过 MTT 测定法、吖啶橙/溴化乙锭（AO/EtBr）荧光染色和 DNA 梯（片段化）测定法对道尔顿淋巴瘤（DL）细胞进行了体外抗癌活性研究。目前的研究表明，铑配合物（4）比钌（1-3）和铱（5）配合物更有效。
