Dual FGFR-targeting and pH-activatable ruthenium-peptide conjugates for targeted therapy of breast cancer.

Dysregulation of Fibroblast Growth Factor Receptors (FGFRs) signaling has been associated with breast cancer, yet employing FGFR-targeted delivery systems to improve the efficacy of cytotoxic agents is still sparsely exploited. Herein, we report four new bi-functional ruthenium-peptide conjugates (RuPCs) with FGFR-targeting and pH-dependent releasing abilities, envisioning the selective delivery of cytotoxic Ru complexes to FGFR(+)-breast cancer cells, and controlled activation at the acidic tumoral microenvironment. The antiproliferative potential of the RuPCs and free Ru complexes was evaluated in four breast cancer cell lines with different FGFR expression levels (SKBR-3, MDA-MB-134-VI, MCF-7, and MDA-MB-231) and in human dermal fibroblasts (HDF), at pH 6.

Design and Anticancer Properties of New Water-Soluble Ruthenium-Cyclopentadienyl Complexes.

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(TPPMS)(L)] [CFSO], where TPPMS = diphenylphosphane-benzene-3-sulfonate, for = 2, L is an imidazole-based ligand (imidazole, 1-benzylimidazole, 1-butylimidazole, (1-(3-aminopropyl)imidazole), and (1-(4-methoxyphenyl)imidazole)), and for = 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.

Experimental data on novel Fe(III)-complexes containing phenanthroline derivatives for their anticancer properties.

This dataset is related to the research article entitled "May iron(III) complexes containing phenanthroline derivatives as ligands be prospective anticancer agents?" [1]. It includes the characterization by UV-Vis absorption spectroscopy and magnetic techniques of a group of mixed ligand Fe(III) complexes bearing a tripodal aminophenolate ligand L, HL = ,-bis(2-hydroxy-3,5-dimethylbenzyl)--(2-pyridylmethyl)amine, and different aromatic bases (NN = 2,2'-bipyridine [Fe(L)(bipy)]PF (), 1,10-phenanthroline [Fe(L)(phen)]PF (), or a phenanthroline derivative co-ligand: [Fe(L)(amphen)]NO (), [Fe(L)(amphen)]PF (), [Fe(L)(Clphen)]PF (), [Fe(L)(epoxyphen)]PF () (where amphen = 1,10-phenanthroline-5-amine, epoxyphen = 5,6-epoxy-5,6-dihydro-1,10-phenanthroline, Clphen = 5-chloro-1,10-phenanthroline), as well as [Fe(L)(EtOH)]NO (), [Fe(phen)Cl] () and [Fe(amphen)Cl] (). Data on their hydrolytic stability in physiological buffers is shown, as well as on their interaction with DNA by spectroscopic tools.

May iron(III) complexes containing phenanthroline derivatives as ligands be prospective anticancer agents?

We report the design, synthesis and biological studies on a group of mixed ligand Fe(III) complexes as anti-cancer drug candidates, namely their interaction with DNA, cytotoxicity and mechanism(s) of action. The aim is to obtain stable, efficient and selective Fe-complexes to be used as anti-cancer agents with less damaging side effects than previously reported compounds. Five ternary Fe(III) complexes bearing a tripodal aminophenolate ligand L, HL = N,N-bis(2-hydroxy-3,5-dimethylbenzyl)-N-(2-pyridylmethyl)amine, and different aromatic bases NN = 2,2'-bipyridine [Fe(L)(bipy)]PF (1), 1,10-phenanthroline [Fe(L)(phen)]PF (2), or a phenanthroline derivative co-ligand: [Fe(L)(amphen)]NO (3), [Fe(L)(amphen)]PF (3a), [Fe(L)(Clphen)]PF (4), [Fe(L)(epoxyphen)]PF (5) (where amphen = 1,10-phenanthroline-5-amine, epoxyphen = 5,6-epoxy-5,6-dihydro-1,10-phenanthroline, Clphen = 5-chloro-1,10-phenanthroline) and the [Fe(L)(EtOH)]NO (6) complex are synthesized.

Antitumour and Toxicity Evaluation of a Ru(II)-Cyclopentadienyl Complex in a Prostate Cancer Model by Imaging Tools.

Background: Ruthenium complexes have been extensively investigated for their prospective value as alternatives to cisplatin. Recently, we reported the in vitro anticancer properties of a family of organometallic ruthenium( II)-cyclopentadienyl complexes and have explored their mechanism of action.

Objective: The purpose of this study was to evaluate the in vivo antitumour efficacy and toxicity of one of these Ru(II) compounds, [RuCp(mTPPMSNa)(2,2'-bipy)][CF3SO2] (TM85) which displayed an interesting spectrum of activity against several cancer cells.

Tracking antitumor metallodrugs: promising agents with the Ru(II)- and Fe(II)-cyclopentadienyl scaffolds.

Research on the field of metal complexes for the treatment of cancer diseases has attracted increasing interest due to the urgency in finding more efficient and selective treatments. Owing to their wide structural diversity, organometallic complexes appear as potential alternatives to the design of new anticancer candidates. Herein, we review recent progress in our work toward the development of new drugs based on Ru(II)- and Fe(II)-cyclopentadienyl scaffolds.

Spraying food sources with pyrethroid to control peridomestic triatomines.

Introduction: We attempted to supplement traditional insecticide spraying by treating peridomiciliar food sources with a powder formulation.

Methods: Two groups of houses were treated with deltamethrin suspension concentrate (SC), one of which had its primary peridomestic food sources treated with deltamethrin 2P.

Results: Triatoma brasiliensis was the most commonly captured triatomine.

First polymer "ruthenium-cyclopentadienyl" complex as potential anticancer agent.

d-glucose end-capped polylactide ruthenium cyclopentadienyl complex (RuPMC) was newly synthesized by a straightforward method. RuPMC was tested against human MCF7 and MDAMB231 breast and A2780 ovarian adenocarcinoma revealing IC50 values in the micromolar range. A pH dependent hydrolysis is advanced by preliminary UV-visible spectroscopy.

Cellular uptake mechanisms of an antitumor ruthenium compound: the endosomal/lysosomal system as a target for anticancer metal-based drugs.

Previous studies have described promising antitumor activity of an organometallic Ru(II) complex, η⁵-cyclopentadienyl(2,2'-bipyridyl)(triphenylphosphane) Ruthenium(II) triflate ([η⁵-C₅H₅)Ru(2,2'-bipyridyl)(PPh₃)][CF₃SO₃]) herein designated as TM34. Its broad spectrum of activity against a panel of human tumor cell lines and high antiproliferative efficiency prompted us to focus on its mode of action. We present herein results obtained with two human tumor cell lines A2780 and MDAMB231 on the compound distribution within the cell, the mechanism of its activity, and its cellular targets.

Crystal structure and experimental and theoretical studies of the second-order nonlinear optical properties of salts of triphenylguanidine with carboxylic acids.

N,N',N''-triphenylguanidinium carboxylate salts have been prepared by acid-base reactions of triphenylguanidine with formic, benzoic, and m-methoxybenzoic acids, and their single-crystal X-ray structure analysis has been performed. The salts were found to crystallize into noncentrosymmetric structures with an orthorhombic space group P2(1)2(1)2(1) for the formate and m-methoxybenzoate salts and a monoclinic space group Cc for the benzoate salt. The anions and cations are linked by intermolecular hydrogen bonds with the same motifs in the three salts.

Occurrence and variability of Panstrongylus lutzi in the State of Ceará, Brazil.

Panstrongylus lutzi is generally restricted to the "caatinga" areas of north-eastern Brazil. Adult insects are frequently found in local houses, but colonies have not previously been registered in the statistics of the Control Programme of Chagas Disease. In Ceará State, our study revealed increasing occurrence of this species, usually with high infection rates for Trypanosoma cruzi, and always represented by adults that invaded the artificial environment.