A new series of 2,4-diamino pyrimidine derivatives with a sulfone-substituted pyrazole right side-chain were discovered as potent anaplastic lymphoma kinase inhibitors. Structure–activity relationship of the left side-chain on phenyl substitutions were explored which delivered many potent ALK i...
The adsorption geometry of Ag(1 1 1)–(√7×√7)R19.1°-4Ar was studied using low-energy electron diffraction (LEED). This higher-order commensurate phase was produced by preadsorbing a small amount of CO in order to block the close-packed steps, which pin the rotation angle of the overlayer. Th...
Resveratrol (RV) 1, a plant polyphenol, has proven effective in commercial products yet drawbacks include low bioavailability due to rapid metabolism. Structural modifications have led to a 4′-acetoxy analog 2 (4AR) now produced using a selective one-step esterification reaction. The one-step s...
Novel silybin acylated derivatives with dicarboxylic acids were prepared in various organic solvents using immobilized Candida antarctica lipase B (Novozym 435®). The reaction parameters affecting the silybin conversion, such as the nature of the organic solvent and the acyl donor used were inve...
Biosynthesis of oleochemicals from lipids and fatty acids draws large attention due to growing interest in natural products and greener processes. Recent developments in biotransformation and biocatalysis based on synthetic biology, metabolic engineering, and enzyme engineering enable us to enha...
Treatment of rats by β,β'-methyl-substituted hexadecanedioic acid (MEDICA 16) resulted in a dose- and time-dependent increase in liver peroxisomal enoyl-CoA hydratase and cyanide-insensitive palmitoyl-CoA oxidation with a concomitant increase in the volume density of peroxisomes as determ...
Development of a 99mTc-fatty acid analogue is of interest, as 99mTc is logistically advantageous over the cyclotron-produced 11C and 123I. Synthesis of a 16 carbon fatty acid derivative and its radiolabeling with the novel [99mTcN(PNP)]2+ core is described here. Hexadecanedioic acid was conjugat...
Not only short chain ω-hydroxycarboxylic acids, α,ω-dicarboxylic acids, and ω-aminocarboxylic acids but also medium to long chain carboxylic acids are widely used as building blocks and intermediates in the chemical, pharmaceutical, and food industries. Thereby, recent achievements in biolog...
Adipic acid is a platform chemical, and is the most important commercial dicarboxylic acid. It has been targeted for biochemical conversion as an alternative to present chemical production routes. From the perspective of bioeconomy, several kinds of raw material are of interest including the sug...
Rat liver acetyl-CoA carboxylase activity was inhibited by the free as well as the CoA monothioester of β,β'-methylsubstituted hexadecanedioic acid (MEDICA 16) (Bar-Tana, J., Rose-Kahn, G. and Srebnik, M. (1985) J. Biol. Chem. 260, 8404–8410 (1985). (1) The CoA monothioester of MEDICA 16...
1.1. A method for the synthesis of the mono-L-carnitine ester of hexadecanedioic acid (hexadecanedioylcarnitine) is described. A thin-layer chromatography system for the separation of long-chain monocarboxylic and long-chain dicarboxylic acylcarnitines was developed.2.2. Hexadecanedioic acid can...
In this paper, we report first, a new synthesis of bis(2-methoxy-4-((E)-prop-1-enyl)phenyl)oxalate, namely, C22H22O6, (I). Then, we present detailed FTIR, 1H NMR, 13C NMR spectroscopies and single-crystal X-ray diffraction techniques, Hartree-Fock (HF) and Density Functional Theory (DFT) molecul...
Two new compounds 1-(4-tert-butyl-benzenesulfonyl)-4-[5-(4-methoxy-phenyl)-[1,3,4]oxadiazol-2-yl]-piperazine (I) and 1-[5-(4-methoxyphenyl)-[1,3,4]oxadiazol-2-yl]-4-[(4-bromo)benzene sulfonyl]-piperazine (II) of 1-[5-(4-methoxy-phenyl)-[1,3,4]oxadiazol-2-yl]- piperazine derivatives have been syn...
SummaryBy feeding of gibberellic acid (GA3) the number of specialized crystal cells in the leaves of the jackbean, Canavalia ensiformis DC., is greatly reduced. If calcium is fed into the stems together with GA3, then the influence of the GA3 on crystal cell differentiation is partly neutralized...
Developing countries are under the clutch of malnutrition due to a lack of protein rich food. Protein supply can be broadened by exploration and exploitation of alternative legume sources. Even though many wild legume landraces have been identified, their utilization is limited due to insufficie...
A new series of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as dual inhibitors of sodium glucose co-transporter proteins (SGLTs) were disclosed. Two methods were developed to efficiently synthesize C5-fluoro-lactones 3 and 4, which are key intermediates to the...
Glutamine (Gln) and its analogues may serve as imaging agents for tumor diagnosis using positron emission tomography (PET), especially for tumors with negative [18F]FDG scan. We report the first automated synthesis of [18F](2S,4R)-4-fluoroglutamine ([18F]FGln) on a GE TRACERlab™ FX-N Pro module....
The reactions of levulinic acid and its pseudo esters, which are readily available from carbohydrate-containing raw materials, with various C-nucleophiles are described. Different reaction pathways were demonstrated depending on the nature of the leaving groups and nucleophiles. For 5-methyl-5-m...
In a preliminary article, we reported the potent allosteric enhancer activity at the A1 adenosine receptor of a small series of 2-amino-3-(4-chlorobenzoyl)-4-[4-(aryl)piperazin-1-yl)methyl]thiophene derivatives bearing electron-withdrawing or electron-releasing groups at the para-position of the...
AimDesign and synthesis of novel nalidixic acid derivatives of potent anticancer and topoisomerase II inhibitory activities were our major aim.
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