Structure determination and investigation on cytotoxicity of potassium dichlorido(l-prolinato)platinate(II) versus chlorido(dimethyl sulfoxide)(l-prolinato)platinum(II) complex - In vitro antitumor deactivation by Cl/dmso ligand exchange

Potassium dichlorido(l-prolinato)platinate(II), K[PtCl₂(l-pro_H)] (1), and chlorido(dimethyl sulfoxide)(l-prolinato)platinum(II), [PtCl(l-pro_H)(dmso)] (2), were synthesized by ligand substitution reactions. Both complexes were characterized by ¹H, ¹³C, and ¹⁹⁵Pt NMR spectroscopy, elemental analysis, and HR-ESI-MS. The molecular structures of 1 and 2 were determined by single crystal X-ray diffraction, proving bidentate coordinated l-prolinato ligand and SP-4-4 configuration of 2a. With the help of DFT calculations stability of possible isomers of 1 and 2 was studied. A considerable difference in the in vitro cytotoxicity of 1 versus 2a (exchange of one chlorido ligand by dmso) against four human cancer cell lines was found.     

Click functionalized poly(p-phenylene ethynylene)s as highly selective and sensitive fluorescence turn-on chemosensors for Zn2+ and Cd2+ ions

Side-chain functionalized poly(p-phenylene ethynylene)s (PPEs) carrying triazole linkers, amino donors/receptors, and solubilizing groups have been found to yield remarkably high efficiency of fluorescence turn-on sensing for Zn(2+) and Cd(2+) ions in THF, and for H(+) and Cd(2+) ions in water.     

Novel transition metal complexes of 4-hydroxy-coumarin-3-thiocarbohydrazone: pharmacodynamic of Co(III) on rats and antimicrobial activity

A new series of stable transition metal complexes of the formula M(L)X·S, where M = Cu(II), Ni(II), Co(III), Cr(III) and Fe(III) and L is the deprotonated ligand of 4-hydroxy-coumarin-3-thiocarbohydrazone, X = Cl(-), NO(3)(-) or CH(3)COO(-) and S = H(2)O and/or EtOH. The HL ligand was prepared by the reaction of 3-formyl-4-hydroxy-coumarine with thiocarbohydrazide in the molar ratio 1:1. The HL ligand and its metal complexes were characterized by elemental analysis, (1)H NMR, IR and electronic spectra, and molar conductance and magnetic measurements and thermal gravimetric analysis (TGA). The HL ligand acts as a monobasic tridentate ONS donor in all metal complexes, and coordinated through the phenolic OH, azomethine nitrogen and thione sulfur. Electronic spectra with magnetic moments suggested varieties of geometries around the central metal atoms. Thermal gravimetric analysis indicates that the complexes are stable up to 300°C, and release the uncoordinated and/or coordinated H(2)O/solvent molecules, which is accompanied by a color change. The formed complexes after releasing the solvent were investigated and their structures are suggested to have square planar or octahedral arrangement. Pharmacodynamic of cobalt(III) complex on some biochemical parameters and histological studies in serum and heart tissue in rats have been studied. Although the complexes demonstrated a significant effect at low dose than the high dose, the ligand showed significant good effects in both high and low doses on the biochemical analysis in serum and heart tissue. Cobalt complex was screened in order to evaluate its antifungal activity against the filamentous fungi Aspergillus niger, Aspergillus fumigatus, and Aspergillus flavus, and antibacterial activity against the Candida albicans, Escherichia coli, Klebseilla pneumoniae and Pseudomonas aeruginosa.     

Development and evaluation of a 166holmium labelled porphyrin complex as a possible therapeutic agent

Porphyrins are interesting derivatives with low toxicity, tumor avidity and rapid wash-out suggested as potential radiopharmaceuticals in radiolabeled form. In this work, [¹⁶⁶Ho] labeled 5,10,15,20-tetrakis(phenyl) porphyrin ([¹⁶⁶Ho]-TPP) was prepared using [¹⁶⁶Ho]HoCl₃ and 5,10,15,20-tetrakis(phenyl)porphyrin (H₂TPP) for 12 h at 50 °C (radiochemical purity: >95 ± 2 % ITLC, >99 ± 0.5 % HPLC, specific activity: 0.9–1.1 GBq/mmol). Stability of the complex was checked in final formulation and human serum for 48 h. The partition coefficient was calculated for the compound (log P = 2.01). The biodistribution of the labeled compound in vital organs of wild-type rats was studied using scarification studies and SPECT. A detailed comparative pharmacokinetic study performed for ¹⁶⁶Ho cation and [¹⁶⁶Ho]-TPP performed up to 24 h. The complex is mostly washed out from the circulation through kidneys and in less extends from the liver. The kidney:blood, kidney:liver and kidney:muscle ratios 4 h post injection were 14, 3.6 and 7.38 respectively.     

Organophosphorus Chemistry,Part 37: Synthesis and Insecticidal Activities of Some Phosphonate Adducts Derived from 6-(Aryliminomethyl)-furobenzopyran-5-ones

Dialkyl phosphites attack 6-(Aryliminomethyl)furobenzopyran-5-ones at the imine-carbon atom to give new phosphonate 1:1 adducts. The obtained compounds regenerate the starting materials upon thermolysis under reduced pressure. Structures of the new products were attested by compatible analytical and spectroscopic measurements. Insecticidal activity tests assured that some new compounds show marked potency against adults of Aphis gossypii (Glover), which infests cotton crops.

Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.     

Near-optimal controls of differential systems with switching and random jumps subject to fast switching and wideband noise perturbation

This work develops near-optimal controls for systems given by differential equations with wideband noise and random switching. The random switching is modeled by a continuous-time, time-inhomogeneous Markov chain. Under broad conditions, it is shown that there is an associated limit problem, which is a switching jump diffusion. Using near-optimal controls of the limit system, we then build controls for the original systems. It is shown that such constructed controls are nearly optimal.     

The synthesis of unsubstituted cyclic imides using hydroxylamine under microwave irradiation

Unsubstituted cyclic imides were synthesized from a series of cyclic anhydrides, hydroxylamine hydrochloride (NH2OH.HCl), and 4-N,N-dimethylamino-pyridine (DMAP, base catalyst) under microwave irradiation in monomode and multimode microwaves. This novel microwave synthesis produced high yields of the unsubstituted cyclic imides for both the monomode (61 - 81%) and multimode (84 - 97%) microwaves.     

Shielding properties of lead and barium phosphate glasses

P₂O₅–PbO–BaO glass system has been investigated to see its potential use as radiation shielding material by studying the effect of the content of each of its composing oxides. The results show that this glass system is suitable as radiation shielding material and has some advantages comparing to the existing commonly used radiation protection glasses.     

Flotation separation and electrothermal atomic absorption spectrometric determination of thallium in wastewater samples

The proposed method is a simple process for the determination of trace amount of thallium(I) in the environmental wastewater samples by electrothermal atomic absorption spectrometry. The wastewater samples were obtained from the environment of a cement plant and subjected to a simple treatment, such as adjusting pH and masking the interfering ions, to prepare for the flotation process in which the thallium(I) content was floated as an ion-association complex using iodide and Rhodamine B at the interface of aqueous/cyclohexane layers. The floated layer was then separated and dissolved in 2 ml of a solution, which was 1% to H2SO4 and 50% to methanol, respectively. Aliquots of 10-microl of this solution were subjected to the graphite furnace to determine the thallium(I) content. The flotation process can be carried in a weak acidic medium in which the interfering effects owing to certain metal ions were eliminated by masking them as neutral citrate chelates. The dynamic range for the determination was found to be 1.0 x 10(-8) - 1.0 x 10(-7) mol l(-1). The RSD was 3.2% and the DL was 2.5 x 10(-9) mol l(-1) (calculated as 3SD of the blank). The reliability of the method is demonstrated by the analysis of a synthetic wastewater in which the recovery was found to be 94%.