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Design,synthesis,characterization,cytotoxic and structure activity relationships of novel Ru(Ⅱ) complexes

Chinese Chemical Letters 2015年第6期26卷 721-726页

作者： Sreekanth Thota Srujana Vallala rajeshwar yerra Eliezer J.Barreiro National Institute for Science and Technology on Innovation on Neglected Diseases (INCT/IDN) Center for Technological Development in Health (CDTS)Fundao Oswaldo CruzMinistério da SadeAv.Brasil 4036Prédio da Expanso8° AndarSala 814Manguinhos21040-361 Rio de JaneiroRJBrazil Programa de Desenvolvimento de Frmacos Instituto de Ciências BiomédicasUniversidade Federal do Rio de Janeiro S.R. College of Pharmacy Department of Pharmaceutical Chemistry & Toxicology

Platinum containing compounds have shown antineoplastic potential, but their clinical applications have been limited by high toxicity. Ruthenium containing complexes have long been known to be well suited for biological applications, and have long been utilized as replacements to popular platinum based-drugs. Here, we report a novel series of ruthenium（ll） arene compounds bearing thiosemicarba- zone and isonicotinylhydrazone ligands with potent anticancer activity their structure activity relationships and apoptosis was studied. The cytotoxic activity of the new ruthenium（ll） arene compounds has been evaluated in several cell lines （Molt 4/C8, LI 210, CEM, HL60 and BEL7402）. Among them, ten complexes were found to be excellent in vitro growth inhibitory activity against various cell lines with IC50 in the sub-micromolar range.

关键词： Cytotoxic Ligand Ruthenium compounds Structure activity relationships

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Synthesis,spectroscopic characterization and in vitro antitumor activities of some novel mononuclear Ru(Ⅱ) complexes

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Chinese Chemical Letters 2012年第4期23卷 466-469页

作者： Sreekanth Thota Mohammad Imran Manasa Udugula rajeshwar yerra Subhas S.Karki Jan Balzarini Erik De Clercq Department of Pharmaceutical Chemistry&Toxicology S.R.College of Pharmacy.Ananthasagar Warangal 506371Andhra Pradesh.India Department of Pharmaceutical Chemistry KLES College of PharmacyRajajinagarBangalore 560010India Rega Institute for Medical Research Katholieke Universiteit Leuven.Minderbroedersstraat 10.B-3000 Leuven.Belgium

The synthesis and spectroscopic characterization of ruthenium complexes（R-l to R-8） of the type[Ru（A）2（B）],（where A = 1,10-phenanthroline/2,2′-bipyridine and B = 3.4.5-tri-OCH_3DPC,4-CH3-DPC,4-N-（CH3）2-DPC,4-NO2-DPC arc described. These ligands form bidentate octahedral ruthenium *** title complexes were subjected to in vitro cytotoxic activity measurements against the human cancer T-lymphocyte cell lines MTT *** vitro evaluation of these ruthenium complexes revealed cytotoxic activity from 0.24 to 1.4μg/mL against CEM,0.44 to 1.9μg/mL against Molt4/C8.0.28 to 1.5μg/mL against L1210,0.24 to 0.98μg/mL against HL60,and 0.25 to 1.2μg/mL against BEL7402,depending the nature of the compound.

关键词： Ruthenium complexes Leukemia cells MTT assay

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