Design, synthesis, and docking studies of phenylpicolinamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors.

Four series of phenylpicolinamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety (12a-e, 13a-f, 14a-f and 15a-i) were designed, synthesized and evaluated for the IC50 values against three cancer cell lines (A549, PC-3 and MCF-7) and c-Met kinase. Five selected compounds (13b, 15b, 15d, 15e and 15f) were further evaluated for the activity against HepG2 and Hela cell lines. Eighteen of the compounds showed excellent cytotoxicity activity and selectivity with the IC50 valuables in single-digit μM to nanomole range.

Quantitative and fingerprinting analysis of Pogostemon cablin based on GC-FID combined with chemometrics.

In this study, a simple, sensitive and reliable gas chromatography-flame ionization detection (GC-FID) method is established for quantitative chemical fingerprinting of essential oils from Pogostemon cablin. Oil samples are prepared by hydrodistillation, with yields ranging from 0.73% to 2.

Recombinant expression, purification, and characterization of an acyl-CoA binding protein from Aspergillus oryzae.

Objectives: To characterize biochemically the lipid metabolism-regulating acyl-CoA binding protein (ACBP) from the industrially-important fungus Aspergillus oryzae.

Results: A full-length cDNA encoding a candidate ACBP from A. oryzae (AoACBP) was cloned and expressed in Escherichia coli as a maltose-binding protein (MBP) fusion protein.

Biotransformation of swertiamarin by Aspergillus niger.

The biotransforamtion of swertiamarin has been carried out using Aspergillus niger. The results showed that 60% swertiamarin were metabolized into two metabolites during the 5 days of biotransformation. The metabolites were identified as erythrocentaurin and 5-ethylidene-8-hydroxy-3,4,5,6,7,8-hexahydro-1Hpyrano[3,4-c]-pyridine-1-one, a novel alkaloid, with NMR and MS.

Design, Synthesis, Activity and Docking Study of Sorafenib Analogs Bearing Sulfonylurea Unit.

Two series of novel sorafenib analogs containing a sulfonylurea unit were synthesized and their chemical structures were confirmed by ¹H-NMR, ¹³C-NMR, MS spectrum and elemental analysis. The synthesized compounds were evaluated for the cytotoxicity against A549, Hela, MCF-7, and PC-3 cancer cell lines. Some of the compounds showed moderate cytotoxic activity, especially compounds 1-(2,4-difluorophenylsulfonyl)-3-(4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea (6c) and 1-(4-bromophenylsulfonyl)-3-(4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea (6f) with the IC50 values against four cancer cell lines ranging from 16.

Solvent effects on electrosynthesis, morphological and electrochromic properties of a nitrogen analog of PEDOT.

A new nitrogen analog of 3,4-ethylenedioxythiophene (EDOT), N-methyl-3,4-dihydrothieno[3,4-b][1,4]oxazine (MDTO), was electropolymerized in different solvents (deionized water, acetonitrile, and propylene carbonate) using LiClO4 as the electrolyte. The structure and performance of as-prepared PMDTO polymers were systematically studied by cyclic voltammetry, UV-vis spectroscopy, FT-IR, SEM, thermogravimetry, spectroelectrochemistry and electrochromic techniques. To our surprise, solvents had a major influence on the electropolymerization of MDTO and properties of the resultant polymers, including morphology, electrochemistry, electronic and optical properties, and electrochromics, etc.

Cordycepin Decreases Compound Action Potential Conduction of Frog Sciatic Nerve In Vitro Involving Ca (2+) -Dependent Mechanisms.

Cordycepin has been widely used in oriental countries to maintain health and improve physical performance. Compound nerve action potential (CNAP), which is critical in signal conduction in the peripheral nervous system, is necessary to regulate physical performance, including motor system physiological and pathological processes. Therefore, regulatory effects of cordycepin on CNAP conduction should be elucidated.

A review of biodegradable polymeric systems for oral insulin delivery.

Currently, repeated routine subcutaneous injections of insulin are the standard treatment for insulin-dependent diabetic patients. However, patients' poor compliance for injections often fails to achieve the stable concentration of blood glucose. As a protein drug, the oral bioavailability of insulin is low due to many physiological reasons.

Multi-functional ion-sensor based on a photochromic diarylethene with a 1H-imidazo [4,5-f][1,10] phenanthroline unit.

A new asymmetrical diarylethene containing a 1H-imidazo [4,5-f][1,10] phenanthroline unit was synthesized. The compound showed typical photochromism and functioned as a notable fluorescence switch upon alternating irradiation with ultraviolet (UV) and visible light. Its closed-ring isomer could be used as a selective 'naked-eye' colorimetric sensor for Cu(2+), accompanied by a notable color change from blue to colorless.

Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors.

Two series of thienopyrimidine derivatives (10a-k, 16a-j) bearing chromone moiety were designed and synthesized. All the compounds were evaluated for inhibitory activity against mTOR kinase at a concentration of 10uM. Four selected compounds were further evaluated for the IC50 values against mTOR kinase, PI3Kα kinase and two cancer cell lines.

Fixation of sulfur dioxide into small molecules.

Sulfonyl-derived functional groups can be found in a broad range of natural products, pharmaceuticals, and materials. Among the methods for the introduction of the sulfonyl group into small molecules, the approach using sulfur dioxide is the most promising and attractive one. In the past several years, the insertion of sulfur dioxide into small molecules under transition metal catalysis or metal-free conditions via a radical process has been developed.

Influence of trace elements mixture on bacterial diversity and fermentation characteristics of liquid diet fermented with probiotics under air-tight condition.

Cu2+, Zn2+, Fe2+ and I- are often supplemented to the diet of suckling and early weaning piglets, but little information is available regarding the effects of different Cu2+, Zn2+, Fe2+ and I- mixtures on bacteria growth, diversity and fermentation characteristics of fermented liquid diet for piglets. Pyrosequencing was performed to investigate the effect of Cu2+, Zn2+, Fe2+ and I- mixtures on the diversity, growth and fermentation characteristics of bacteria in the liquid diet fermented with Bacillus subtilis and Enterococcus faecalis under air-tight condition. Results showed that the mixtures of Cu2+, Zn2+, Fe2+ and I- at different concentrations promoted Bacillus growth, increased bacterial diversity and lactic acid production and lowered pH to about 5.

Concise total synthesis of two marine natural nucleosides: trachycladines A and B.

We report the first total synthesis of trachycladines A (10 steps, 34.2% overall yield) and B (11 steps, 35.0% overall yield) by using 5-deoxy-1,2,3-tri-O-acetyl-β-D-ribofuranose as the starting material.

Preparation of camptothecin-loaded targeting nanoparticles and their antitumor effects on hepatocellular carcinoma cell line H22.

Camptothecin (CPT) is an effective anticancer agent against various cancers but the clinical application is limited because of its poor water solubility, low bioavailability and severe toxic side effects. The aim of the present study was to evaluate the feasibility of using targeted NPs as a high-performance CPT delivery system that targets liver cancer cells through intravenous (i.v.

Many local pattern texture features: which is better for image-based multilabel human protein subcellular localization classification?

Human protein subcellular location prediction can provide critical knowledge for understanding a protein's function. Since significant progress has been made on digital microscopy, automated image-based protein subcellular location classification is urgently needed. In this paper, we aim to investigate more representative image features that can be effectively used for dealing with the multilabel subcellular image samples.

Neuroprotection against Aβ25-35-induced apoptosis by Salvia miltiorrhiza extract in SH-SY5Y cells.

The neurotoxicity of β-amyloid protein (Aβ) contributes significantly to the pathogenesis of Alzheimer's disease (AD), and hence the attractive therapeutic strategies focusing on the modulation of Aβ-induced neurotoxicity are warranted. The present study aims to investigate the neuroprotection and underlying mechanisms by which Salvia miltiorrhiza Bunge (Lamiaceae) extract (SME) protects against Aβ25-35-induced apoptosis in SH-SY5Y cells. 2h Pre-treatment of SH-SY5Y cells with SME (0.

Carbon nanofibers modified graphite felt for high performance anode in high substrate concentration microbial fuel cells.

Carbon nanofibers modified graphite fibers (CNFs/GF) composite electrode was prepared for anode in high substrate concentration microbial fuel cells. Electrochemical tests showed that the CNFs/GF anode generated a peak current density of 2.42 mA cm(-2) at a low acetate concentration of 20 mM, which was 54% higher than that from bare GF.

(2R,3S,4R,5R)-5-(4-Amino-5-iodo-7H-pyrrolo-[2,3-d]pyrimidin-7-yl)-4-fluoro-2-(hy-droxy-meth-yl)tetra-hydro-furan-3-ol.

The title compound, C11H12FIN4O3, is composed of a 7-carbapurine moiety connected via an N atom to 2-de-oxy-2-fluoro-β-d-ribose. The conformation about the N-glycosydic bond is -anti with χ = -129.0 (11)°.

Absolute configurations of new limonoids from a Krishna mangrove, Xylocarpus granatum.

Four new limonoids, named granatumins V-Y (1-4), belonging to the small group of limonoids with a C1-C29 oxygen bridge and a ∆(8,30) double bond, were isolated from the seeds of an Indian mangrove, Xylocarpus granatum, collected in the swamp of Krishna estuary, Andhra Pradesh. The constitutions and absolute configurations of these compounds were established by extensive NMR investigations, single-crystal X-ray crystallography using Cu Kα radiation, and by the comparison of circular dichroism spectrum.

2,2,2-Tri-fluoro-N-(2-iodo-phen-yl)acetamide.

The three F atoms in the title compound, C8H5F3INO, are disordered over two sets of sites [relative occupancies = 0.615 (14):0.385 (14)].

Ethyl N-(3-cyano-1H-indol-2-yl)form-imidate.

In the title compound, C12H11N3O, the C=N imino bond is in an E conformation. In the crystal, adjacent mol-ecules are linked by N-H⋯Ncyano hydrogen bonds, forming a chain running along [110].

Amphiphilic chitosan derivative-based core-shell micelles: synthesis, characterisation and properties for sustained release of Vitamin D3.

Novel amphiphilic chitosan derivative of N,N-dimethylhexadecyl carboxymethyl chitosan (DCMCs) was synthesised. The physical properties of DCMCs were characterised by Fourier transform-infrared spectroscopy, nuclear magnetic resonance spectroscopy, X-ray diffraction and differential scanning calorimetry. DCMCs can form core-shell micelles with low critical micelle concentration (31 mg L(-1)).

Pluronic P85/poly(lactic acid) vesicles as novel carrier for oral insulin delivery.

Poly(lactic acid)-b-Pluronic-b-poly(lactic acid) (PLA-P85-PLA) vesicles were developed as novel carrier for oral insulin delivery. PLA-P85-PLA block copolymer was synthesized by ring opening polymerization of the monomer l-lactide using Pluronic copolymer P85 as the initiator. Insulin-loaded PLA-P85-PLA vesicles were prepared by dialysis method and the mean diameter of insulin-loaded PLA-P85-PLA vesicles was determined to be 178 nm.

A silver(I)-catalyzed tandem reaction of 2-alkynylbenzaldoximes with ketenes.

A novel and unexpected reaction of 2-alkynylbenzaldoximes with ketenes in the presence of silver triflate (10 mol%) under mild conditions is discovered. This reaction proceeds through 6-endo-cyclization, [3 + 2] cycloaddition, and rearrangement, leading to isoquinoline derivatives in moderate to good yields.