Synthesis, characterisation and DNA intercalation studies of regioisomers of ruthenium (II) polypyridyl complexes.

Title Synthesis, characterisation and DNA intercalation studies of regioisomers of ruthenium (II) polypyridyl complexes.
Authors L. Perdisatt; S. Moqadasi; L. O'Neill; G. Hessman; A. Ghion; M.Qasim Mush Warraich; A. Casey; C. O'Connor
Journal J Inorg Biochem
DOI 10.1016/j.jinorgbio.2018.01.018
Abstract

Regioisomers of the functional group of the main ligand (L) on a series of [Ru(phen)L]and [Ru(bpy)L] complexes, where phen is 1,10 phenanthroline and bpy is 2,2'-bipyridine, were synthesised to investigate the interaction with deoxyribonucleic acid (DNA) as potential therapeutics. UV-Vis binding titrations, thermal denaturation and circular dichroism were used to evaluate their interaction with DNA. The conclusions indicated the significance of the auxiliary ligand; especially 1,10-phenanthroline has on the binding constants (K). The systematic variation of auxiliary ligand(phen or bpy), and polypyridyl ligand (4-(1H-Imidazo[4,5-f][1,10]phenanthrolin-2-yl)benzonitrile (CPIP), 2-(4-formylphenyl)imidazo[4,5-f] [1,10] phenanthroline (FPIP), 2-(4-bromophenyl)imidazo[4,5-f][1,10]phenanthroline (BPIP) and 2-(4-nitrophenyl)imidazo[4,5-f] [1,10] phenanthroline (NPIP), split in terms of functional group change were investigated for DNA interaction. The CPIP analogues in particular were investigated for the regioisomerism (ortho, meta, para) effect of the nitrile group on the ligand. It was found that both the DNA interaction could be tailored through the systematic variation of the electronic nature of the individual auxiliary ligand and to a lesser extent the functional group and regioisomeric change. Preliminary cell line studies have been carried out to determine the selectivity of the complexes against cell lines such as A375 (Skin Cancer), HeLa (Cervical Cancer), A549 (Lung Cancer), Beas2B (Lung Normal Cell) and MCF-7 (Breast Cancer). Complexes which had strong DNA interactions in the binding studies have proven to be the most efficacious against certain cell lines. Establishing well-defined structure property relationships when looking at trends in spectroscopic properties and DNA binding will aid in the intelligent design of potential therapeutic complexes.

Citation L. Perdisatt; S. Moqadasi; L. O'Neill; G. Hessman; A. Ghion; M.Qasim Mush Warraich; A. Casey; C. O'Connor.Synthesis, characterisation and DNA intercalation studies of regioisomers of ruthenium (II) polypyridyl complexes.. J Inorg Biochem. 2018;182:7182. doi:10.1016/j.jinorgbio.2018.01.018

Related Elements

Ruthenium

See more Ruthenium products. Ruthenium (atomic symbol: Ru, atomic number: 44) is a Block D, Group 8, Period 5 element with an atomic weight of 101.07. Ruthenium Bohr ModelThe number of electrons in each of ruthenium's shells is [2, 8, 18, 15, 1] and its electron configuration is [Kr] 4d7 5s1. The ruthenium atom has a radius of 134 pm and a Van der Waals radius of 207 pm. Ruthenium was discovered by Jędrzej Śniadecki in 1807. It was first recognized as a distinct element by Karl Ernst Claus in 1844. Elemental RutheniumIn its elemental form, ruthenium has a silvery white metallic appearance. Ruthenium is a rare transition metal belonging to the platinum group of metals. It is found in pentlandite, pyroxenite, and platinum group metal ores. The name Ruthenium originates from the Latin word "Ruthenia," meaning Russia.

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