. The Fe or Ru organometallic π-donor fragments were linked by an extended π system to the acceptor Cr(CO) 3 fragment. The effect of π back-donation involving the second Fe or Ru metal centre and the π* orbitals of the NϵC-coordinated group, was probed by the ν (NϵC) stretching bands on the IR spectra and also by NMR spectroscopic data. The planarity, largely due
2015): A new ruthenium cyclopentadienyl azole compound with activity on tumor cell lines and trypanosomatid parasites, Journal of Coordination Chemistry, As part of our efforts to develop organometallic ruthenium compounds bearing activity on both trypanosomatid parasites and tumor cells, a new Ru(II)-cyclopentadienyl clotrimazole complex, [RuCp(PPh 3 ) 2 (CTZ)](CF 3 SO 3 ) where Cp = cyclopentadienyl, CTZ = clotrimazole, was synthesized and characterized. The compound was evaluated in vitro on T. cruzi (Y strain), the infective form of T. brucei brucei strain 427 (cell line 449), on three human tumor cell lines with different sensitivity to cisplatin (A2780, ovary; MCF7, breast; HeLa, cervix) and on J774 murine macrophages as mammalian cell model. The new compound is more cytotoxic on T. cruzi and on the tumor cell lines than the reference drugs (Nifurtimox and cisplatin, respectively). In addition, complexation of the bioactive CTZ to the {RuCp(PPh 3 )} leads to significant increase of the antiparasitic and antitumoral activity. To get insight into the potential "dual" mechanism of antiparasitic action emerging from the presence of Ru(II) and CTZ in a single molecule, the inhibitory effect of this new complex on the biosynthesis of T. cruzi sterols of membrane and the interaction with DNA were studied. Although the tested complex does not affect DNA, it affects the T. cruzi biosynthetic pathway of conversion of squalene to squalene oxide. According to the results here reported, [RuCp(PPh 3 ) 2 (CTZ)][CF 3 SO 3 ] could be considered a prospective antiparasitic and/or antitumoral agent that deserves further evaluation.
INTRODUÇÃOAtualmente, a enfermagem passa por uma situação caracterizada pelo abandono de muitos profissionais, devido a vários fatores, entre eles destacam-se as más condições de trabalho e a baixa remuneração. Tal situação vem se refletindo na qualidade da assistência de enfermagem e na satisfação de seus profissionais.
Ruthenium complexes are emerging as one of the most promising classes of complexes for cancer therapy. However, their limited aqueous solubility may be the major limitation to their potential clinical application. In view and to contribute to the progress of this field, eight new water-soluble Ru(II) organometallic complexes of general formula [RuCp(mTPPMS)n(L)] [CF3SO3], where mTPPMS = diphenylphosphane-benzene-3-sulfonate, for n = 2, L is an imidazole-based ligand (imidazole, 1-benzylimidazole, 1-butylimidazole, (1-(3-aminopropyl)imidazole), and (1-(4-methoxyphenyl)imidazole)), and for n = 1, L is a bidentate heteroaromatic ligand (2-benzoylpyridine, (di(2-pyridyl)ketone), and (1,2-(2-pyridyl)benzo-[b]thiophene)) were synthesized and characterized. The new complexes were fully characterized by NMR, FT-IR, UV–vis., ESI-HRMS, and cyclic voltammetry, which confirmed all the proposed molecular structures. The antiproliferative potential of the new Ru(II) complexes was evaluated on MDAMB231 breast adenocarcinoma, A2780 ovarian carcinoma, and HT29 colorectal adenocarcinoma cell lines, showing micromolar (MDAMB231 and HT29) and submicromolar (A2780) IC50 values. The interaction of complex 6 with human serum albumin (HSA) and fatty-acid-free human serum albumin (HSAfaf) was evaluated by fluorescence spectroscopy techniques, and the results revealed that the ruthenium complex strongly quenches the intrinsic fluorescence of albumin in both cases.
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