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Probing the antibacterial and anticancer potential of tryptamine based mixed ligand Schiff base Ruthenium(III) complexes
Institution:1. Bioinorganic Lab., Department of Chemistry, Jamia Millia Islamia, New Delhi 110025, India;2. Department of Inorganic and Physical Chemistry, Indian Institute of Science, Bangalore 560012, India;3. Medicinal Chemistry Lab., Department of Biosciences, Jamia Millia Islamia, New Delhi 110025, India;4. Chemistry Department, Faculty of Science, University of Jeddah, P.O. Box 80327, Jeddah 21589, Saudi Arabia;1. H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;2. Centre for Advanced Drug Research (CADR), Department of Pharmacy COMSATS Institute of Information Technology, Abbottabad, Pakistan;3. Department of Biochemistry, Computational Medicinal Chemistry Laboratory, UCSS, Abdul Wali Khan University Mardan, Pakistan;4. Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 31441, Dammam, Saudi Arabia;5. PCSIR Laboratories Complex, Karachi, Shahrah-e-Dr. Salimuzzaman Siddiqui, Karachi 75280, Pakistan;6. Département de Microbiologie-infectiologie et d''immunologie, Faculté de Médecine, Université Laval, Québec, QC G1V 0A6, Canada;7. Centre de Recherche du CHU de Québec-Université Laval, Québec, QC G1V 4G2, Canada;8. Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia;1. Faculty of Applied Sciences, Universiti Teknologi MARA, 40450 Shah Alam, Selangor, Malaysia;2. Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300 Bandar Puncak Alam, Selangor, Malaysia;3. Collaborative Drug Discovery Research (CDDR) Group, Pharmaceutical and Life Sciences Community of Research, Universiti Teknologi MARA (UiTM), 40450 Shah Alam, Selangor, Malaysia;4. Faculty of Science and Technology, Universiti Sains Islam Malaysia, Bandar Baru Nilai, 71800 Nilai, Negeri Sembilan, Malaysia;5. Atta-ur-Rahman Institute for Natural Product Discovery (AuRIns), UiTM Puncak Alam, Selangor, Malaysia;1. Department of Chemistry, Sri Sairam Engineering College, Chennai 600 044, Tamil Nadu, India;2. Department of Chemistry, K.V., DGQA, Chennai 600 114, Tamil Nadu, India;1. Departamento de Química, Instituto de Ciências Exatas e Naturais do Pontal, Universidade Federal de Uberlândia, Rua vinte, 1600, CEP 38304-402, Ituiutaba, MG, Brazil;2. Instituto de Química, Universidade Federal de Goiás, Avenida Esperança, s/n, Campus Samambaia, CEP 74690-900, Goiânia, GO, Brazil;3. Instituto de Química de São Carlos, Universidade de São Paulo, CP 780, 13560-590 São Carlos, SP, Brazil;4. Departamento de Química, Universidade Federal do Paraná, Centro Politécnico, CP 19081, Curitiba, PR, Brazil;5. Departamento de Química, Instituto Tecnológico de Aeronáutica, Comando-Geral de Tecnologia Aeroespacial, São José dos Campos, São Paulo 12228-900, Brazil;1. Seethalakshmi Ramaswami College, Trichy;2. Research Department of Chemistry, Seethalakshmi Ramaswami College, Trichy
Abstract:Development of new chemotherapeutic agents to treat microbial infections and recurrent cancers is of pivotal importance. Metal based drugs particularly ruthenium complexes have the uniqueness and desired properties that make them suitable candidates for the search of potential chemotherapeutic agents. In this study, two mixed ligand Ru(III) complexes Ru(Cl)2(SB)(Phen] (RC-1) and Ru(Cl)2(SB)(Bipy)] (RC-2) were synthesised and characterized by elemental analysis, IR, UV–Vis, 1H, 13C NMR spectroscopic techniques and their molecular structure was confirmed by X-ray crystallography. Antibacterial activity evaluation against two Gram-positive (S. pneumonia and E. faecalis) and four Gram-negative strains (P. aurogenosa, K. pneumoniae, S. enterica, and E. coli) revealed their moderate antibacterial activity with MIC value of ≥250 μg/mL. Anticancer activity evaluation against a non-small lung cancer cell line (H1299) revealed the tremendous anticancer activity of these complexes which was further validated by DNA binding and docking results. DNA binding profile of the complexes studied by UV–Visible and fluorescence spectroscopy showed an intercalative binding mode with CT-DNA and an intrinsic binding constant in the range of 3.481–1.015× 105 M?1. Both the complexes were also found to exert weak toxicity to human erythrocytes by haemolytic assay compared to cisplatin. Potential of these complexes as anticancer agents will be further delineated by in vivo studies.
Keywords:Ru(III) complexes  X-ray crystallography  Antimicrobial  DNA binding  Anticancer  Docking
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