The reference standards methyl 4-(2-methyl-5-(methoxycarbamoyl)phenylamino)-5-methylpyrrolo[2,1-f][1,2,4]triazine-6-carboxylate (10a), methyl 4-(2-methyl-5-(ethoxycarbamoyl)phenylamino)-5-methylpyrrolo[2,1-f][1,2,4]triazine-6-carboxylate (10b) and corresponding precursors 4-(2-methyl-5-(methoxyc...
Blockade of the interleukin-6 receptor (IL-6R) is a successful therapeutic strategy in various inflammatory diseases. IL-6 can signal via membrane-bound (classic signaling) and soluble forms (sIL-6R, trans-signaling) of the IL-6R. Trans-signaling is causative for the pro-inflammatory properties ...
For centuries Danggui Longhui Wan has been used to treat chronic ailments, such as myelocytic leukemia. In the 1960s, the active ingredient in Danggui Longhui Wan was isolated and identified as indirubin. Indirubin has shown potent inhibition of cyclin-dependent kinase through binding to the ATP...
Microstructure and unit sequence are critical parameters that determine the properties of polybutadiene materials. In this contribution, we have reported the syntheses, characterization of 6-(di-tert-butyl-phosphine) amine fused 2-R-pyridine compounds (R = 1′H-oxazoline (L1); 4′,4′-dimethyl o...
An expeditious stereoselective synthesis of sex pheromone (±)3,5-cis-dimethyl-6-trans-isopropyl-3,4,5,6-tetrahydropyran-2-one of larval parasitoid M. grandii, from readily available isobutyraldehyde and furan is described.
Infrared spectra (3200–220 cm−1) of gaseous and Raman spectra (3200–40 cm−1) of liquid isopropyl isocyanide ((CH3)2CHNC) have been recorded. By utilizing the microwave rotational constants combined with the structural parameters predicted from MP2(full)/6-311+G(d,p) calculations, adjusted r0 p...
BackgroundFalse-positive blood cultures can lead to unnecessary risks and misuse of antibiotics; to reduce rates of false-positives, it would be useful to determine whether use of an antiseptic with a prolonged effect is required.
cis-6-Hexadecenoic acid is a major component of human sebaceous lipids that is involved in skin self-sterilization and atopic dermatitis amelioration. It can be prepared by hydrolysis of isopropyl cis-6-hexadecenoate produced by resting cells of Rhodococcus sp. strain KSM-MT66. To devise an econ...
The d-methionine- and 2-methyl-dl-methionine analogs of the enzymatic methyl donor, (−)S-adenosyl-l-methionine, were synthesized by methylation of S-adenosyl-d-homocysteine and S-adenosyl-2-methyl-dl-homocysteine with methyl iodide. By chromatographic purification, S-adenosyl-d-methionine and S-...
Supplementation of the culture medium of Candida utilis with d-methionine or 2-methyl-dl-methionine leads to intracellular synthesis of S-adenosyl-d-methionine and S-adenosyl-2-methylmethionine. The identity of the sulfonium compounds was established by tracer technique, chromatography, acid hyd...
SummaryS-Adenosyl-(±)-2-methylmethionine, an inhibitor of mammalian S-adenosyl-L-methionine decarboxylase, inhibited the increase in [3H]-thymidine incorporation but did not interfere with the rise in [3H]-uridine and [3H]-leucine incorporation induced by concanavalin A in cultured mouse lympho...
Covalent attachment of poly(ionic liquid)s (PILs) by click chemistry on glass or silicon (Si) surfaces was performed. Poly[1-(4-vinylbenzyl)-3-butylimidazolium bis(trifluoromethylsulfonyl)imide] (polyVBBI+Tf2N−), and copolymers of polyVBBI+Tf2N− with fluorescein O-methacrylate were synthesized b...
Patients with major depressive disorder have elevated peripheral inflammation; the degree of this increase correlates with the severity of the disorder. Chronic psychological stress increases pro-inflammatory cytokines and promotes microglial activation, leading to stress vulnerability. Epigenet...
Toxicity of vanadium on cells is one of the less studied effects. This prompted us to study the structural effects induced on neuroblastoma and erythrocytes by vanadium (V) sodium metavanadate. This salt was incubated with mice cholinergic neuroblastoma cells and intact human erythrocytes. To le...
The present study describes anticancer effect of gallic acid based indanone derivative (1). Indanone 1 exhibited in vivo anticancer activity against Erhlich ascites carcinoma in Swiss albino mice by inhibiting tumor growth by 54.3% at 50 mg/kg b.wt. It showed antitubulin effect by inhibiting tub...
An electronic tuning Nazarov-type cyclization protocol was proposed for the synthesis of polysubstituted-1-indanones from the readily available starting materials 1,4-enediones. AlCl3 was highlighted as the most efficient promoter for this reaction.
In an attempt to discover a potent and selective anticancer agent, gallic acid has been modified to benzylidene indanones as tubulin polymerization inhibitors. These compounds were evaluated against several human cancer cell lines and also evaluated for inhibition of tubulin polymerase in in vit...
3-(3′,4′,5′-Trimethoxyphenyl)-4,5,6-trimethoxy,2-(3″,4″-methylenedioxybenzylidene)-indan-1-one (1) is an optimized anti-cancer lead molecule obtained on modification of gallic acid, a plant phenolic acid. It exhibited potent cytotoxicities (IC50 = 0.010–14.76 μM) against various human car...
2-(Arylthio)thiophenes, 2-(alkylthio)thiophene, and 2-(thiophenylthio)thiophene were prepared in high yield by simply mixing 2-iodothiophene and aryl, alkyl, or thienyl thiols at room temperature without solvent, base, and/or catalyst.
A copper-mediated synthesis of diaryl sulfides utilizing Cu(I)-thiophene-2-carboxylate (CuTC) is described. We demonstrate the use of CuTC as a soluble, non-basic catalyst in the coupling of aryl iodides and aryl thiols in the synthesis of synthetically advanced diaryl sulfides. This method allo...
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