Literature DB >> 18614238

Synthesis, characterization, X-ray structure and in vitro antimycobacterial and antitumoral activities of Ru(II) phosphine/diimine complexes containing the "SpymMe2" ligand, SpymMe2=4,6-dimethyl-2-mercaptopyrimidine.

Fábio B do Nascimento1, Gustavo Von Poelhsitz, Fernando R Pavan, Daisy N Sato, Clarice Q F Leite, Heloisa S Selistre-de-Araújo, Javier Ellena, Eduardo E Castellano, Victor M Deflon, Alzir A Batista.   

Abstract

The reaction of cis-[RuCl(2)(dppb)(N-N)], dppb=1,4-bis(diphenylphosphino)butane, complexes with the ligand HSpymMe(2), 4,6-dimethyl-2-mercaptopyrimidine, yielded the cationic complexes [Ru(SpymMe(2))(dppb)(N-N)]PF(6), N-N=bipy (1) and Me-bipy (2), bipy=2,2'-bipyridine and Me-bipy=4,4'-dimethyl-2,2'-bipyridine, which were characterized by spectroscopic and electrochemical techniques and X-ray crystallography and elemental analysis. Additionally, preliminary in vitro tests for antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27264 and antitumor activity against the MDA-MB-231 human breast tumor cell line were carried out on the new complexes and also on the precursors cis-[RuCl(2)(dppb)(N-N)], N-N=bipy (3) and Me-bipy (4) and the free ligands dppb, bipy, Me-bipy and SpymMe(2). The minimal inhibitory concentration (MIC) of compounds needed to kill 90% of mycobacterial cells and the IC(50) values for the antitumor activity were determined. Compounds 1-4 exhibited good in vitro activity against M. tuberculosis, with MIC values ranging between 0.78 and 6.25microg/mL, compared to the free ligands (MIC of 25 to >50microg/mL) and the drugs used to treat tuberculosis. Complexes 1 and 2 also showed promising antitumor activity, with IC(50) values of 0.46+/-0.02 and 0.43+/-0.08microM, respectively, against MDA-MB-231 breast tumor cells.

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Year:  2008        PMID: 18614238     DOI: 10.1016/j.jinorgbio.2008.05.009

Source DB:  PubMed          Journal:  J Inorg Biochem        ISSN: 0162-0134            Impact factor:   4.155


  4 in total

Review 1.  Targeting InhA, the FASII enoyl-ACP reductase: SAR studies on novel inhibitor scaffolds.

Authors:  Pan Pan; Peter J Tonge
Journal:  Curr Top Med Chem       Date:  2012       Impact factor: 3.295

2.  A Nanostructured Lipid System to Improve the Oral Bioavailability of Ruthenium(II) Complexes for the Treatment of Infections Caused by Mycobacterium tuberculosis.

Authors:  Patricia B da Silva; Eduardo Sinésio de Freitas; Mariana Cristina Solcia; Paula Carolina de Souza; Monize Martins da Silva; Alzir Azevedo Batista; Carlos E Eismann; Ana Marta C M Rolisola; Amauri A Menegário; Rosilene Fressatti Cardoso; Marlus Chorilli; Fernando R Pavan
Journal:  Front Microbiol       Date:  2018-12-06       Impact factor: 5.640

3.  In vitro and in vivo activities of ruthenium(II) phosphine/diimine/picolinate complexes (SCAR) against Mycobacterium tuberculosis.

Authors:  Fernando R Pavan; Gustavo V Poelhsitz; Lucas V P da Cunha; Marilia I F Barbosa; Sergio R A Leite; Alzir A Batista; Sang H Cho; Scott G Franzblau; Mariana S de Camargo; Flávia A Resende; Eliana A Varanda; Clarice Q F Leite
Journal:  PLoS One       Date:  2013-05-28       Impact factor: 3.240

4.  Novel Zinc(II) Complexes [Zn(atc-Et)₂] and [Zn(atc-Ph)₂]: In Vitro and in Vivo Antiproliferative Studies.

Authors:  Erica de O Lopes; Carolina G de Oliveira; Patricia B da Silva; Carlos E Eismann; Carlos A Suárez; Amauri A Menegário; Clarice Q F Leite; Victor M Deflon; Fernando R Pavan
Journal:  Int J Mol Sci       Date:  2016-05-21       Impact factor: 5.923

  4 in total

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