Direct asymmetric aldol reactions between 4-nitrobenzaldehyde and cyclohexanone were catalysed by trans-4-hydroxy-(S)-prolinamide (10 mol %) in the presence of CH3COOH (10 mol %) as the co-catalyst under solvent-free conditions at 15 °C. (2S,4R)-4-Hydroxy-N-((S)-1-phenylethyl)pyrrolidine-2-carb...

1,2,3-Triazolium salts draw much attentions in recent years. We developed a new synthetic method to heteroatom-functionalized triazoliums via nucleophilic substitution of 4-bromomethyltriazolium. This method afforded triazoliums with different S, N, and O heteroatom-substituents. Moreover, SN2′...

The epidermal growth factor receptor represents an important target in cancer therapy, and low molecular weight inhibitors based on quinazolines have reached the marked. Herein we report on a new scaffold, 5-aryl-7H-pyrrolo[2,3-d]pyrimidin-4-amines, and show that when employing (S)-phenylglycino...

On irradiation of solutions of polyfluorinated aryloxo-1,2-dihydronaphthalenes and 6-phenyl-3-phenoxy-2,4-cyclohexadienone, the main reaction pathway is cyclization leading to polyfluorinated benzonaphtho- and dibenzo-furans.

This paper investigates the effects of anisole and methyl acetate (as fuel additives) on the performance and emission characteristics of a compression-ignition (i.e., diesel) engine. Anisole and methyl acetate can be obtained from methylation of phenol and acetic acid, respectively. Phenol and a...

The thermal decomposition of three methyl anisole isomers (o-, m-, and p-methyl anisole) were investigated to understand the influences of methyl substitution position on the benzene ring at low pressure (below 15 Pa) within temperature range from 473 to 1473 K. The pyrolytic phenomena were stud...

2-Arylidene-4-(4-phenoxy-phenyl)but-3-en-4-olides (1–17) were prepared from 3-(4-phenoxy-benzoyl)propionic acid and aromatic aldehydes. Some of the selected butenolides were reacted with ammonia and benzylamine to give corresponding 3-arylidene-5-(4-phenoxy-phenyl)-2(3H)-pyrrolones (18–23) and...

Organophosphonates are a group of chemical agents which have high bioactivity. In the present study, we aimed to investigate the anticancer activity of the synthesized β-lactam derivatives of α-amino phosphonates on solid tumor and human leukemic cell lines. The results show that one of these ...

Methyl (E)-(3-(3,4-dihydroxyphenyl)acryloyl)tryptophanate (MHAT) is an O-methyl ester of javamide-II showing strong anti-inflammatory activity. Therefore, in this study, MHAT was chemically synthesized, and its effects on p38 MAP kinase, NF-κB, and monocyte chemotactic factor-1 (MCP-1) expressi...

A series of novel (E)-3-(3,4-dihydroxyphenyl)acrylylpiperazine derivatives had been synthesized and evaluated their biological activities as potential tubulin polymerization inhibitors. Among these compounds, compound 3q exhibited potent antiproliferative activities against three cancer cell lin...

Acid-activated clays KSF and KSF/0 were successfully used in the hydrogen peroxide conversion of phenyl acetic acid to high-added phenolic compounds: p-hydroxyphenyl acetic acid and 3,4-dihydroxyphenyl acetic acid, endowed with a powerful antioxidant capacity. The catalytic conversion enhancemen...

Phosphoric and phosphorous acid esters have been applied to surface oxidized Co–Cr thin films, and their lubrication performances are investigated. Tricresyl phosphate, phosphoric and phosphorous acid esters with long alkyl chains are found to be very effective in reducing friction and wear of ...

A ‘green’ ARGET-ATRC, for the CuCl[PMDETA] catalysed cyclo-isomerization of N-allyl-α-polychloroamides to γ-lactams is described. The process works efficiently (yields 78–96%), uses a bio-solvent, as ethanol, and exploits the reducing feature of ascorbic acid to limit, at a low level (2–4%...

γ-Hydroxybutyratic acid (GHB), and its prodrugs 4-butyrolactone and 1,4-butanediol, represent expanding drugs of abuse, although GHB is also used therapeutically to treat narcolepsy and alcoholism. Thus, the pathway by which GHB is metabolized is of importance. The goal of the current study was...

Alpha-keto acids are the deaminated form of amino acids, which have been used in several applications in the medicine, food, and feed industries. In vivo, alpha-keto acids are ketogenic or glucogenic precursors, which regulate protein turnover. Since alpha-keto acids do not have amino groups, su...

The photocatalyzed degradation and mineralization of branched C4 and C5 acids {2-methylpropanoic acid (2-MPA), 2-methylbutanoic acid (2-MBA), 3-methylbutanoic acid (3-MBA), and trimethylacetic acid (TMA)} and oxidized C4 and C5 carboxylic acids {e.g., 2-hydroxybutanoic acid (2-HBA), 2-hydroxy-2-...

Insulin-releasing effects of straight and branched chain 2-keto acids were assessed using clonal glucose-responsive β-cells. Pyruvic acid (PA), 2-ketovaleric acid (KV), 2-ketoisovaleric acid (KIV) or 2-keto-3-methylvaleric acid (KMV) dose-dependently promoted the stimulatory effects of D-glucos...

8-Methoxypsoralen (8-MOP) is a well established drug in the treatment of various skin diseases. Pretreatment of mice with 8-MOP before administration of 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) significantly reduced the incidence of NNK-induced tumor. The present study was designed t...

Although allogeneic hematopoietic progenitor cell transplant (HPCT) is curative therapy for many disorders, it is associated with significant morbidity and mortality, which can be related to graft-versus-host disease (GVHD) and the immunosuppressive measures required for its prevention and/or tr...

L-leucyl-L-leucine methyl ester (LLME) prevents GVHD in several animal models by depleting dipeptidyl peptidase I (DPPI)-expressing cytotoxic cellular subsets. However, clinical application has been hampered by difficulties in stem cell engraftment following treatment of donor bone marrow inocul...