title: Heteroleptic arene Ru(II) dipyrrinato complexes: DNA, protein binding and anti-cancer activity against the ACHN cancer cell line.
abstract: 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 ).
authors.affiliation: Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi 221 005, U.P., India. dspbhu@bhu.ac.in.
authors.forename: Rakesh Kumar
authors.initials: RK
authors.lastname: Gupta
authors.affiliation: Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi 221 005, U.P., India. dspbhu@bhu.ac.in.
authors.forename: Amit
authors.initials: A
authors.lastname: Kumar
authors.affiliation: Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi 221 005, U.P., India. dspbhu@bhu.ac.in.
authors.forename: Rajendra Prasad
authors.initials: RP
authors.lastname: Paitandi
authors.affiliation: Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi 221 005, U.P., India. dspbhu@bhu.ac.in.
authors.forename: Roop Shikha
authors.initials: RS
authors.lastname: Singh
authors.affiliation: Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi 221 005, U.P., India. dspbhu@bhu.ac.in.
authors.forename: Sujay
authors.initials: S
authors.lastname: Mukhopadhyay
authors.affiliation: Centre for Genetic Disorders, Banaras Hindu University, Varanasi 221 005, U.P., India.
authors.forename: Shiv Prakash
authors.initials: SP
authors.lastname: Verma
authors.affiliation: Centre for Genetic Disorders, Banaras Hindu University, Varanasi 221 005, U.P., India.
authors.forename: Parimal
authors.initials: P
authors.lastname: Das
authors.affiliation: Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi 221 005, U.P., India. dspbhu@bhu.ac.in.
authors.forename: Daya Shankar
authors.initials: DS
authors.lastname: Pandey
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002417:Cattle; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004247:DNA / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D062105:Molecular Docking Simulation; D009690:Nucleic Acid Conformation; D009942:Organometallic Compounds / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D011485:Protein Binding; D011487:Protein Conformation; D012428:Ruthenium / Q000737:chemistry*; D012710:Serum Albumin, Bovine / Q000737:chemistry / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D012710:Serum Albumin, Bovine; D012428:Ruthenium; D004247:DNA