PurposeThe response of 2-amino-4-([14C]methylthio)butyric acid ([14C]Met) uptake and [125I]3-iodo-alpha-methyl-l-tyrosine ([125I]IMT) uptake to radiotherapy of C10 glioma cells was compared to elucidate the intracellular reactions that affect the response of 2-amino-4-([11C]methylthio)butyric ac...
Interdiffusion coefficients and molar conductivities of the macrocycle tetrasodium 5,11,17,23-tetrakissulfonatemethylen-2,8,14,20-tetra(2(methylthio)ethyl)resorcinarene (H8Na4RSTio) in non-buffered aqueous solutions at 25.00 °C and at concentrations from (0.001 to 0.020 mol·dm−3) have been mea...
The preparation of neat 1,2,4-tris(methylthio)-3-H-hexafluoro-n-butane is described. The mechanism, which involves the elimination of hydrogen fluoride with the subsequent isomerization in forming the cis- and trans- 1,2,4-tris(methylthio)hexafluoro-l-butene, is discussed. This study also suppor...
The acid–base and the UV behavior of 3-(3,4-dihydroxyphenyl)-propenoic acid (caffeic acid) was studied by potentiometry and UV spectrophotometry at T = 298.15 K and 0.1 ≤ I/mol L− 1 ≤ 1 in NaCl aqueous solution. The complex formation with Zn2 +, Cu2 +, Cd2 +, (CH3)2Sn2 + at I = 0.1 mol L− 1 i...
The present work highlightsthe synthesis of a newer biologically active Mannich bases contributing 4-((4-fluorobenzylidene)amino)-5-(pyridin-4-yl)-4H-1,2,4-triazole-3-thiol and various heterocyclic amines via N-Mannich reaction by the conventional method as well as microwave heating approach as ...
In the present study, two important starting materials and 18 new 1,2,4-triazole compounds with mono ring system have been synthesized and characterized. The mono system showed 16 compounds of a Schiff base moiety attached to the triazole ring which was prepared from the corresponding starting m...
Although mutated Ras protein is well recognized as an important drug target, direct targeting Ras has proven to be a daunting task. Recent studies demonstrated that Ras protein needs PDEδ to relocate to plasma membrane to execute its signaling transduction function, which provides a new avenue ...
A novel type of nucleotide analogues, the 2′,3′-O-(1-diethylphosphono)alkylidene derivatives of ribonucleosides was prepared by redox reaction of diethyl chlorophosphite with various nucleoside orthoesters. Some of these compounds undergo interesting rearrangements when treated with nucleophil...
As a PI3K and mTOR dual inhibitor, N-(2-chloro-5-(2-acetylaminobenzo[d]thiazol-6-yl)pyridin-3-yl)-4-fluorophenylsulfonamide displays toxicity when orally administrated. In the present study, alkylurea moiety replaced the acetamide group in the compound and a series of 1-alkyl-3-(6-(2,3-disubstit...
To affiliate multiple bioactivities in a compact heteronuclei, two series of benzimidazole based 1,3,4-oxadiazoles were synthesized and assessed in vitro for their efficacy as antimicrobial agents against eight bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aerug...
1H,1H,5H-Perfluoropentyl-1,1,2,2-tetrafluoroethylether (F-EAE) mixed with ethylene carbonate (EC), diethyl carbonate (DEC), and lithium hexafluorophosphate (LiPF6) is evaluated as a co-solvent high-potential electrolyte of LiNi1/3Co1/3Mn1/3O2/graphite batteries. Linear sweep voltammetry (LSV) an...
Prompted by the literature report on anticancer properties of mefenamic acid, a series of mefenamic acid based indole derivatives were designed via a rational approach. Synthesis of this class of compounds was carried out via a 3-step method starting from the mefenamic acid and using the Pd/C–C...
An ab initio quantum mechanical study of the conformational preferences of N-methyl-1-(N′-acetylamino)-t-2-phenylcyclohexane-r-1-carboxamide, a cyclic analogue of phenylalanine MeNH-c6Phe-CONHMe), has been performed at the HF/3-21G and HF/6-31G∗ computational levels. Results show a γ-turn geom...
(2R,3Z)-, (2R,3E)-, (2S,3Z) and (2S,3E)-2-Acetylamino-3-octadecen-1-ol, and (2R)- and (2S)-2-acetylamino-octadecan-1-ol were prepared using the Wittig olefination of Garner's aldehyde (N-Boc-N,O-isopropylidene-l- or d-serinal) from l- or d-serine. The apoptotic activities of these saturated...
The radiopharmaceutical 3-[123I]iodo-α-methyl-L-tyrosine ([123I]IMT) can be used to study amino acid transport by single-photon emission tomography (SPET). In order to evaluate the potential contribution of [123I]IMT accumulation in macrophages to overall uptake values measured in neoplastic le...
Nuclear farnesoid X receptor (FXR) has important physiological roles in various metabolic pathways including bile acid, cholesterol and glucose homeostasis. The clinical use of known synthetic non-steroidal FXR ligands is restricted due to toxicity or poor bioavailability. Here we report the dev...
A library of 16 4-substituted 2-(1H-pyrrolo[3,2-c]pyridin-2-yl)propan-2-ols 17–32 has been synthesized for use in biological testing against Trypanosoma cruzi, the protozoan parasite that causes Chagas disease. The 4-substituted 2-(1H-pyrrolo[3,2-c]pyridin-2-yl)propan-2-ols 17–32 were subjecte...
In this study, using a natural and green protein R-phycoerythrin (R-PE) extracted from marine Porphyra yezoensis as the stabilizer and reducer, silver nanoparticles (AgNPs) were synthesized. Based on this, a highly sensitive and selective method for the detection of Cu2+ ions was developed using...
Extraction of phycobiliproteins (R-phycoerythrin, R-PE) from macroalgae is difficult due to the presence of complex matrix of polysaccharides (agar, cellulose etc.) present in the cell wall which offers major hindrance for cell disruption. The present study is focused on the identification of su...
C‑phycocyanin peptide (CPC) grafted N‑succinyl chitosan (NSC) was prepared via the catalysis of Microbial transglutaminase (MTGase). The single factor experiment displayed that the degree of substitution (DS) of N‑succinyl chitosan‑C‑phycocyanin peptide (NSC‑CPC) depended on the reaction time, t...
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