This work aims to characterise the solute-solute interaction which occurs in a ternary system containing CO2 with solutes, 1-decanol and 3,7-dimethyl-1-octanol and to compare the ability of the RK-ASPEN and CPA models, available within the Aspen Plus® software, to predict solubility data for thi...
The synthesis of optically active β-triazolyl amino alcohols was carried out via ruthenium catalyzed asymmetric transfer hydrogenation of α-triazolyl amino alkanones. This reaction proceeds under mild reaction conditions with up to 99% yield and 99.9% enantiomeric excess (ee). This protocol wa...
Retinoic acid-induced heparin binding protein (RIHB) is a highly basic, secreted polypeptide expressed during early chick embryogenesis. We have characterized the binding of 125I-labeled RIHB to embryonal chondrocytes in culture. No saturable, high-affinity binding can be observed on these cells...
Amphiphilic heparin-retinoic acid (HR) and heparin-folate-retinoic acid bioconjugates (HFR) were synthesized by chemical conjugation of a hydrophobic anticancer agent all-trans-retinoic acid (RA) and a targeting ligand, folic acid (FA), to the high molecular weight heparin backbone. The HR and H...
A 19 KDa heparin binding protein was previously purified from chicken embryos. Essentially localized within basement membranes in early embryonic tissues, this protein is very rich in basic and cystein residues. Its N-terminal fragment is similar to corresponding fragment of two other proteins e...
Retinoic acid (all-trans and 9-cis) isomers represent important therapeutic agents for many types of cancers, including human breast cancer. Changes in protein composition of the MCF-7 human breast cancer cells were induced by all-trans retinoic acid, 9-cis retinoic acid, and their combination a...
Since polyphenols are known to exhibit antioxidative properties, we prepared and characterized persimmon vinegar polyphenols (PVP) in this study. Furthermore, we investigated the protective effect of PVP on hydrogen peroxide (H2O2)-induced oxidative stress in HepG2 cells and its underlying mecha...
One of the possible ways for using silver nanoparticles (AgNPs) in spectrophotometry is their application for the determination of oxidizing agents, based on oxidative destruction of these nanoobjects. This process depends on the structure of AgNPs surface layer, which is essentially affected by...
Two novel 4,4′-bis(alkylphenyl/alkyloxyphenyl)-2,2′-bithiophene bridged cyclic thiourea functionalized triphenylamine sensitizers (D8 and D9), comprising 2-cyanoacrylic acid as the acceptor, have been designed and synthesized for dye-sensitized solar cells (DSSCs). For comparison, an analogue ...
ABSTRACTHere, three new 3,4-ethylenedioxythiophene bis-substituted bithiophene containing alkyl side chain groups (alkyl = hexyl, octyl, and dodecyl) comonomers, 5,5′-(4,4′-dihexyl-[2,2′-bithiophene]-5,5′-diyl) bis(2,3-dihydrothieno[3,4-b][1,4]dioxine (BEDOT-BT-BH), 5,5′-(4,4′-dioctyl-[2,2...
A natural product inspired library was synthesized based on 2,3-diarylbenzofuran and 2,3-diaryl-2,3-dihydrobenzofuran scaffolds. The library of forty-eight compounds was prepared by utilizing Pd-catalyzed one-pot multicomponent reactions and ruthenium-catalyzed intramolecular carbenoid C-H inser...
2-Aminobenzophenones and acetophenones were N-acylated with α-azido carboxylic acids to give the corresponding anilides. Reductive cyclization provided 3-substituted-2H-1,4-benzodiazepin-2-ones in good (46–99%) yields.
Procedures for the direct high-performance liquid chromatographic enantiomer separation of four bicyclo[2.2.2]octane-based 3-amino-2-carboxylic acids were developed in polar-ionic mode on zwitterionic chiral stationary phases (CSPs) based on cinchonane alkaloide quinine, quinidine and chiral sul...
Synthesis of 7-heteroaryl-2-azabicyclo[2.2.2]oct-7-enes by cycloaddition and subsequent cross-coupling reaction is described. Binding affinity of these novel compounds towards the characteristic receptorial targets of ibogaine is illustrated.
Fluorinated analogs that are related to the 5-hydroxytryptamine (5-HT1A) antagonist, N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635), have been synthesized and their binding affinity for the 5-HT1A receptor and other neurotransmitter receptors (...
A series of new quinolone-3-carboxylic acids featuring a hydroxyl group at C-5 position were synthesized and evaluated for their in vitro activity against HIV in C8166 cell culture. All the compounds showed anti-HIV-1 activity with low micromolar to submicromolar EC50 values. The most active com...
Angiogenesis is modulated by a multitude of pro-angiogenic factors including VEGFR-2, Tie-2, and EphB4. Moreover, their crosstalk also had been well elaborated. We have identified several diarylurea-based VEGFR-2 inhibitors as potential anti-angiogenesis agents. As a continuation to our previous...
VEGFR-2, TIE-2, and EphB4 are essential for both angiogenesis and tumorigenesis. Herein, we designed and prepared three classes of multi-target inhibitors based on the extensive sequence homology along the kinase domain of angiogenic RTKs. Biological evaluation indicated that these multi-target ...
Synthesis and properties of double-stranded RNAs (dsRNAs) and small interfering RNAs (siRNAs) containing 4′-C-aminoethyl-2′-deoxy-2′-fluorouridine are described. Thermal denaturation studies showed that incorporation of 4′-C-aminoethyl-2′-fluoro analog improved the thermal stabilities of ds...
Malignant ascites (MA) is one of the severe complications of gastrointestinal tumors, affecting the patients’ survival time and quality of life. Euphorbia kansui is a commonly used toxic Chinese herbal medicine for malignant ascites. Our previous study showed that the biological and toxicologic...
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