Protein aggregation via 3D domain swapping is a complex mechanism which can lead to the acquisition of new biological, benign or also malignant functions, such as amyloid deposits. In this context, RNase A represents a fascinating model system, since by dislocating different polypeptide chain re...
3-benzoyl-4-hydroxybenzoic acid (3) was synthesized, spectroscopically characterized and the crystal structure was determined using single crystal X-ray diffraction method. In addition, the thermal studies were carried out using thermogravimetric analysis (TGA). The dihedral angle between phenyl...
The syntheses of ethyl 2-[4-(3-fluoro-2-quinoxalinyloxy)phenoxy]propanoate (1d), a new fluoro analogue of the herbicide quizalofopethyl, from 2,3-dichloroquinoxaline (3) and of ethyl 2-[4-(6-chloro-3,4-dihydro-3-oxoquinoxalinyl-2-oxy)phenoxy]propanoate (9) from ethyl 2-[4-(3,6-dichloro-2-quinoxa...
EGFR inhibitors are well-known as anticancer agents. Quite differently, we report our effort to develop EGFR inhibitors as anti-inflammatory agents. Pyrimidinamide EGFR inhibitors eliciting low micromolar IC50 and the structurally close non-EGFR inhibitor urea analog were synthesized. Comparing ...
Sulfonamide Schiff's base namely, 4-((4-fluoro-3-phenoxybenzylidene) amino) benzene sulfonamide (4-FBABS) has been synthesized from 4-fluoro-3-phenoxybenzaldehyde, 4-aminobenzenesulfonamide and few drops of glacial acetic acid by condensation method and characterized by microanalysis, Fouri...
ObjectiveIntimal hyperplasia (IH) is the main cause of therapeutic failure after vascular and endovascular surgery. However, there is currently no targeted therapy for the treatment of IH. We recently reported that the inhibition of cyclic adenosine monophosphate response element (CRE) binding p...
The 2′,3′-cyclic nucleoside monophosphates (2′,3′-cNMPs) of adenosine, guanosine, cytidine, and uridine were prepared in good yield in a one pot reaction from unprotected ribonucleosides and activated trimetaphosphate in the presence of N-methylimidazole, 4-nitroimidazole and MgCl2.
Over the last decade, there is growing incidence of male reproductive malfunctions. It has been documented that numerous environmental contaminants, such as endocrine disruptors (EDs) may adversely affect the reproductive functions of humans as well as wildlife species. The aim of this in vitro ...
Herein, we propose the synthesis of a microspherical imprinted hydrogel meant for the controlled release of a nucleotide, adenosine 5′-monophosphate (5′-AMP). Indeed, molecularly imprinted polymers-based (MIPs) materials possess remarkable selective molecular recognition ability that mimicks b...
The lattice constants, electronic structure, and optical properties of Gadolinium monophosphate GdPO4 are investigated using the first principles calculations. Our calculated lattice constants are in excellent agreement with the available theoretical and experimental data. Band structure calcula...
The heat capacity function Cp,mo=fT of crystalline CsNiPO4 was measured between 6 K and 650 K. A heat capacity anomaly was found around 382.8 K due to a phase transition. The experimental data obtained were used to calculate the standard thermodynamic functions Cp,mo/R, Δ0THmo/RT, Δ0TSmo/R and...
Graphitic carbon nitride (g-C3N4) doped carboxylated MWCNTs nanocomposite was synthesized using a simple method. The composite films containing 45 wt%, 50 wt%, 56 wt%, 67 wt% fraction of the carboxylated MWCNTs doped into g-C3N4 were fabricated and characterized. An electrochemical non-enzymatic...
The Nanocrystalline cellulose (NCC) was prepared from filter paper by acid hydrolysis process. The modification of NCC with cationic, anionic, and nonionic surfactant did not have a tremendous effect on the chemical structure of material based on the characterization of XRD and FTIR. The modifie...
BackgroundCycloastragenol (CAG), a triterpene aglycone is commonly prescribed for treating hypertension, cardiovascular disease, diabetic nephropathy, viral hepatitis, and various inflammatory-linked diseases.
Four paclitaxel derivatives were afforded by preparative HPLC separation of two pairs of diastereoisomers, which were obtained by catalytic hydrogenation and epoxidation of the C-13 side-chain double bond of cephalomannine, a naturally occurring paclitaxel analog. The four paclitaxel derivatives...
Cancer is the second cause of death worldwide, exceeded only by cardiovascular diseases. The prevalent treatment currently used against metastatic cancer is chemotherapy. Among the most studied drugs that inhibit neoplastic cells from acquiring unlimited replicative ability (a hallmark of cancer...
Activation of cannabinoid CB1 receptors suppresses pathological pain but also produces unwanted side effects, including tolerance and physical dependence. Inhibition of fatty-acid amide hydrolase (FAAH), the major enzyme catalyzing the degradation of anandamide (AEA), an endocannabinoid, and oth...
(S)-3-Methyl-3-butenyl-(2R,3S)-N-benzoyl-3-phenylisoserinate is used as a model of the C-13 side chain, an essential subunit for the cytotoxicity of the diterpenoid paclitaxel, a chemotherapeutic drug used in the treatment of cancer. The potential energy surface (PES), calculated using a density...
Prostate cancer (PC) is the second most commonly occurring cancer in men. Conventional chemotherapy has wide variety of disadvantages such as high systemic toxicity and low selectivity. Targeted drug delivery is a promising approach to decrease side effects of therapy. Prostate specific membrane...
Two spiro paclitaxel-mimics consisting only of an oxetane D-ring and a C-13 side chain were designed and synthesized on the basis of analysis of structure–activity relationships (SAR) of paclitaxel. In vitro microtubule-stabilizing and antiproliferative assays indicated a moderate weaker activi...
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