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...

The enzymatic synthesis of phenolic lipids (PLs) by transesterification of flaxseed oil with 3,4-dihydroxyphenyl acetic acid (DHPA) was investigated in solvent-free medium (SFM), using Novozym 435 from Candida antarctica as the biocatalyst. The effects of selected reaction parameters, water acti...

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...

AimsDanshensu [3-(3,4-dihydroxyphenyl)-lactic acid], a phenylpropanoid compound isolated from Prunella vulgaris var. lilacina, is a well-known antioxidant. Although its antioxidant activity and cardioprotective effect have been reported, the pharmacological properties of danshensu in the central...

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...

Derivatization of the natural compound 3-(3,4-dihydroxyphenyl)-propionic acid (dihydrocaffeic acid) can be achieved by laccase-catalyzed N-coupling of aromatic and aliphatic amines. Incubation of 3-(3,4-dihydroxyphenyl)-propionic acid and 4-aminobenzoic acid with laccase in aqueous medium and in...

A selective methodology for the synthesis of either 3-cyanoindoles or 4-cyanoquinolines via a base-modulated palladium-catalyzed reductive N-heterocyclization from a common 1-cyano-1-(2-nitrophenyl)-1-alkene precursor is described. The required starting materials were prepared either by a Kosugi...

Simplified des-AB-type aglycone of antitumor steroidal saponin OSW-1 was concisely prepared starting from readily available Hajos ketone. We further completed the synthesis of des-AB-OSW-1 analogue by the installation of the disaccharide moiety into the des-AB aglycone, and evaluated its antitum...

Syntheses of 2-(4-carboxybut-1-enyl/4-carboxypent-1-ynyl)cyclopentene-1-carboxamides, compounds designed to mimic the phosphoSer–Pro dipeptide motif (the recognition sequence for the prolyl cis–trans isomerase Pin1), have been developed. Stille, Sonogashira and Suzuki couplings were envisaged ...

This paper describes an improved procedure for the synthesis of racemic myo-inositol 1-(4-nitrophenyl hydrogen phosphate) (NPIP) a useful substrate for the continuous spectrophotometric assay of phosphatidylinositol-specific phospholipase C (PI-PLC).

Thermal evaporating technique was used to prepare 2,9-Bis [2-(4-chlorophenyl)ethyl] anthrax [2,1,9-def:6,5,10-d′e′f′] diisoquinoline-1,3,8,10 (2H,9H) tetrone (Ch-diisoQ) thin films. The studied films were irradiated with gamma rays in the air at room temperature with different absorbed doses ...

Three series of ferrocene containing 3-(arylthio)propan-1-ones (each of eight examples) have been synthesized by thia-Michael addition of the corresponding thiophenols to acryloylferrocene, 1-ferrocenyl-3-phenylprop-2-en-1-one and 3-ferrocenyl-1-phenylprop-2-en-1-one promoted by the catalyst gen...

C6H5SeNa+(generated in situ by NaBH4 reduction of (C6H5Se)2) on reaction with 1-(3-chlorophenyl)-4-(3-chloropropyl) piperazinium chloride under N2 atmosphere results in [1-(3-chlorophenyl)-4-(3-phenylseleno propyl) piperazinium chloride] (LH+Cl−) as cream colour solid. Its anion exchange product...

Tris(2-cyanoethyl)phosphine (tcep) reacts with the copper(I) compounds, CuX (X = Cl, Br, I and SCN), in a 1:1 ratio to give 1:1 complexes, CuX(tcep), whereas it reacts with CuY (Y = PF6, ClO4, NO3, BH4, CN and CF3COO) in a 2:1 ratio to give the 2:1 complexes, CuY(tcep)2. Single crystal X-ray str...

The synthesis and reactions of 1-(N-benzylamino)-1-(2-pyridyl)- and 1-(N-benzylamino)-1-(4-pyridyl)-methyldiphenylphosphine oxides are described. It was found that these compounds were exceptionally easy to cleave in aqueous sulfuric acid solutions to form diphenylphosphinic acid and the corresp...

β-Carboline derivatives are known as the lead compounds for anti-tumor agents. To examine an optimal structure for anti-tumor activity, we synthesized a variety of β-carboline derivatives, possessing a variety of substituents on the nitrogen atom of the amino group of 3-amino-β-carboline, and...

A series of 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones were synthesized using 2-amino-5-nitrophenol as a starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES test) and their neurotoxicity was evaluated by the rotarod neurotoxicity test (Tox.). T...

Many glycosyltransferase inhibitors in the literature are structurally derived from the donor or acceptor substrate of the respective enzyme. A representative example is 2-naphthyl β-d-GlcNAc, a synthetic GlcNAc glycoside that has been reported as a galactosyltransferase inhibitor. This GlcNAc ...

Benzamide derivatives as radiotracers have played an important role in diagnosing malfunction in dopaminergic neurotransmission. A variety of halogenated and two unsubstituted benzamide derivatives were synthesised and their in vitro affinities to dopaminergic, serotonergic and adrenergic recept...

The tide compound was synthesised in the optically active form in seven steps from (4R,6R)-actinol in 34% overall yield. The relative configuration within the C15-key intermediate acetylenic triol, 2-E-5-((1S,4R;,6R)-1,4-dihydroxy-2,2,6-trimethylcyclohexyl)-3-methyl-2- penten-4-yn-1-ol, was dete...