Monatshefte Fur Chemie最新文献

Abstract: Size-exclusion chromatography-inductively coupled plasma-mass spectrometry (SEC-ICP-MS) was used to study the serum-binding preferences of two metallodrugs with anticancer activities in vivo, namely the organoruthenium compound plecstatin-1 and its isosteric osmium analog. The complexes were administered intraperitoneally into mice bearing a CT-26 tumor. Comparing the total metal content of mouse whole blood and serum underlined that the metallodrugs are mainly located in serum and not in the cellular fraction of the blood samples. In mouse serum, both compounds were not only found to bind extensively to the serum albumin/transferrin fraction but also to immunoglobulins. Free drug was not observed in any of the samples indicating rapid protein binding of the metallodrugs. These findings were validated by spiking human serum with the respective compounds ex vivo. An NCI-60 screen is reported for the osmium analog, which revealed a relative selectivity for cancer cell lines of the ovary and the central nervous system with respect to plecstatin-1. Finally, a COMPARE 170 analysis revealed disruption of DNA synthesis as a possible treatment effect of the osmium-based drug candidate.

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Abstract: Some new trans-dihydronarciclasine derivatives containing a 1,4-benzodioxane moiety were stereoselectively synthesised using our feasible and efficient method developed recently. These new phenanthridone alkaloid analogues were obtained in both racemic and optically active forms. High enantioselectivities (up to 99% ee) were achieved by applying (8S,9S)-9-amino(9-deoxy)epiquinine as an organocatalyst. Due to a side reaction, various methoxyphenanthridine regioisomers were also prepared which afforded further synthetic trans-dihydronarciclasine analogues modified in the ring A of the phenanthridone scaffold.

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Abstract: The atomic absorption spectrometry (AAS) method is one of the most accessible procedures for ferrous ions testing in various compositions including pharmaceutical preparations. The aim of the study was to develop and partially validate analytical method which could be an excellent alternative to the routine procedure performed within dissolution studies. Electric conductivity is simple, fast, and hassle-free method. The samples during dissolution process were measured using conductivity probe in entire dissolution assessment protocol. The conductivity results were compared to data obtained from AAS. The dissolution studies were performed according to modified pharmacopoeial standards, in 900 cm³ of purified water as an acceptor medium, at 37 °C, until the achievement of an equilibrium state for every tested composition. Validity study of the developed method confirmed acceptable linearity of obtained calibration plots (r² > 0.9553). Linearity at 100% level was found to be 100.59, 97.49, and 94.82, respectively, for drug compositions A, B, and C. Precision results were 100.45, 95.97, and 95.73, respectively, for A, B, and C, with RSD below 2% between all samples in all above mentioned formulations. The drug composition D hindered the proper validation of the method due to the high variability between samples. The method has acceptable performance features for evaluation of three of four solid drug composition containing ferrous ions.

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Abstract: This review is aimed to provide extensive survey of quinolones and fluoroquinolones for a variety of applications ranging from metal complexes and nanoparticle development to hybrid conjugates with therapeutic uses. The review covers the literature from the past 10 years with emphasis placed on new applications and mechanisms of pharmacological action of quinolone derivatives. The following are considered: metal complexes, nanoparticles and nanodrugs, polymers, proteins and peptides, NO donors and analogs, anionic compounds, siderophores, phosphonates, and prodrugs with enhanced lipophilicity, phototherapeutics, fluorescent compounds, triazoles, hybrid drugs, bis-quinolones, and other modifications. This review provides a comprehensive resource, summarizing a broad range of important quinolone applications with great utility as a resource concerning both chemical modifications and also novel hybrid bifunctional therapeutic agents.

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Abstract: 5-(Nitromethyl)-3-phenyl-4,5-dihydroisoxazole was obtained as a product of a high-yielding [3 + 2] cycloaddition reaction of in situ-generated benzonitrile N-oxide and 3-nitroprop-1-ene. For the first time, the regiochemistry of this reaction was unambiguously proven by X-ray structural analysis. The quantum-chemical calculation performed at the M06-2X/6-31G(d) (PCM) theoretical level affords a basis for explaining the course of reaction as well as the nature of transition states. Next, further DFT calculations together with spectral data shed light on structural aspects of the product.

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Abstract: Sultones, the cyclic esters of hydroxyl sulfonic acids, are a fascinating class of heterocycles and the recent years have witnessed an increasing interest in these molecules, especially in six-ring δ-sultones. The importance of these compounds is either because of their biological properties themselves or due to their versatility as intermediates in more complex target syntheses. Accordingly, the development of new synthesis methods to access δ-sultones is an important and rewarding task which we wish to highlight in this review.

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Abstract: The concise synthesis of a novel chiral diyne substrate for the assembly of chiral naphthylpyridines was described and different conditions for the cobalt-catalyzed co-cyclotrimerization with nitriles investigated. The products are novel naphthylpyridines possessing configurationally stable biaryl axes.

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Abstract: The preparation, structural characterization, luminescence, and catalytic activity of three palladium(II) complexes bearing imino phenoxide ligands are reported. The X-ray studies revealed that the complexes are mononuclear with palladium centres coordinated in a square-planar coordination environment. Two of the complexes are emissive in solution at room temperature. The catalytic activities towards the ring-opening polymerization of rac-lactide (rac-LA) were tested. Polymers with moderate molecular weights and relatively broad dispersity (Ð) were obtained. Kinetic studies revealed that the polymerization followed first-order kinetics.

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Abstract: Citrus fruits are very popular food products. There are many species and varieties of them. There are also documented cases of some citrus fruits causing a severe allergic reaction. Some species of the citrus fruits, especially hybrid ones show a reduced allergenic effect due to the lack of seeds. There is a need for rapid methods for evaluation of citrus' botanical origin. During research, the headspace of three citrus fruits Citrus Aurantifolia, Citrus japonica, and Citrus × floridana was analysed using electronic nose based on ultrafast gas chromatography and gas chromatography with mass spectrometry. In the paper, two approaches were compared. The usefulness of an electronic nose to control the quality of hybrids was demonstrated. The results obtained during ultrafast gas chromatography analyses were subjected to statistical analysis. Four chemometric methods namely: principal component analysis (PCA), discriminant function analysis (DFA), soft independent modeling of class analogies (SIMCA), statistical quality control (SQC) were used to distinguish between limequat and its parent fruits. Electronic nose combined with chemometrics is a novel analytical tool for hybrid fruits' classification due to their botanical origin. It can supplement established techniques by providing results in a short time and at a low cost.

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Abstract: The quality of the fruit is affected by several main ingredients and the aroma plays a fundamental role during the selection of fruit by consumers. In the case where several fruit have similar aromas and only one of them has specific health properties, it is very important to find the differences in the volatile organic compounds (VOCs) composition to distinguish these samples. Such situations are often found for hybrid fruit. Sweetie is a hybrid of grapefruit and pummelo. Sweetie fruit is characterized by high antioxidant potential and a positive effect on human health. The aim of this study was to verify the unique volatile compositional traits of three species of citrus fruit. Proton transfer reaction Time-of-Flight mass spectrometry (PTR-TOF-MS) was utilized to obtain the mass-resolved fingerprints of VOCs. The chemical formula of these VOC masses was tentatively identified. Principal component analysis was performed to evaluate the differences between the groups.

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