Transcription factor E1AF is widely known to play critical roles in tumor metastasis via directly binding to the promoters of genes involved in tumor migration and invasion. Here, we reported for the first time the pro-apoptotic role of E1AF in tumor cells. The expression of E1AF at protein leve...

Mithramycin (also known as Plicamycin) is an antineoplastic antibiotic produced by Streptomyces plicatus. Mithramycin A is a DNA/RNA polymerase inhibitor, DNA-binding transcriptional inhibitor, antibiotic, and observed to facilitate tumor necrosis factor (TNF)-α and Fas ligand-induced apoptosis...

Activation of peripheral nociceptors by products of inflammation has been shown to be dependent on specific sensory transducing elements such as the capsaicin receptor, TRPV1. The development of high-affinity antagonists to TRPV1 as well as to other receptors capable of detecting noxious stimuli...

PurposeSpecificity protein 1 (SP1) is involved in the transcription of several genes implicated in tumor maintenance. We investigated the effects of mithramycin A (MTA), an inhibitor of SP1 DNA binding, on radiation response.

A two-step protocol for the synthesis of 5-substituted or 5,6-disubstituted furo[2,3-d]pyrimidines using bifunctional electrophiles and a pyrimidine derivative was developed. The first step is O-alkylation of 2-methylthiopyrimidin-4,6-dione utilizing bifunctional electrophiles which are readily ...

Beta-N-methylamino-L-alanine (BMAA) is a non-proteinogenic amino acid produced by several cyanobacteria species. It is considered to be a potent neurotoxin. Although its neurotoxic effects are well studied, other negative effects of BMAA have not yet been completely elucidated. In the present st...

Human dietary exposure to the environmental neurotoxin β-N-methylamino-L-alanine (BMAA) has been implicated in an increased risk of developing sporadic neurodegenerative diseases like Alzheimer's and amyotrophic lateral sclerosis. Evidence suggests that humans are exposed to BMAA globally,...

β-N-methylamino-L-alanine (BMAA) and 2,4-diaminobutyric acid (DAB) are two newly identified algal toxins, and they may react with chlorine to undergo decomposition and generate disinfection byproducts (DBPs) during pre-chlorination as well as chlorine disinfection. In this study, the decomposit...

Bioaccumulation and biomagnification of β-N-methylamino-L-alanine (BMAA), a potent neurotoxin, has been demonstrated in various food webs. It is alarming as this intensification of BMAA will result in exposure to higher concentrations from a direct cyanobacterial source. As more food items are ...

Cycad-associated neurodegenerative disease is more strongly correlated with the gymnosperm's major neurotoxin cycasin (methylazoxymethanol glucoside) than with the minor neurotoxin β-N-methylamino-L-alanine (L-BMAA).

The interactions of avarone, a quinone from the marine sponge Dysideaavara, and the methylamino derivatives of avarone (2), 3′-(methylamino)avarone (3) and 4′-(methylamino)avarone (4) with calf thymus DNA (CT-DNA) were studied. Agarose gel electrophoreticanalysis showed that binding of the qui...

RésumeLa constante de première acidité du 7-para carboxy anilino-4-nitrobenzofurazane noté 4H,COOH, dans le diméthylsulfoxyde a été estimée par un dosage RMN.Le diacide 4H,COOH a été préparé par simple réaction de substitution nucléophile aromatique (SNAr) et le sel monopotassique ...

An efficient method for the synthesis of 1,7-dithia-3,5-diazacycloalkan-4-ones and 1,7-dithia-3,5-diazacycloalkane-4-thiones has been developed via the cyclothiomethylation reaction of (thio)urea with bis(N,N-dimethylamino)methane and α,ω-alkanedithiols such as 1,2-ethanedithiol, 1,3-propanedi...

To achieve the synthesis of (R)-bambuterol, a prodrug of (R)-terbutaline, asymmetric reduction of 1-[3,5-bis(dimethylcarbamoyloxy)phenyl]-2-chloroethanone with whole cells of Williopsis californica JCM 3600 pre-incubated on glycerol as a carbon source was examined. Initially, the insolubility of...

A number of 3,5-bis(benzylidene)-4-piperidones 1 and some N-4-(2-aminoethoxy)phenylcarbonyl analogs 3–6 display excellent in vitro antimycobacterial properties. In particular, 1c and 6d are potent antimycobacterials which are well tolerated in mice and are identified as important lead molecules...

Two novel series of dimeric 3,5-bis(arylidene)-4-piperidones 7 and 8 were prepared as cytotoxic agents. A specific objective of this study was the discovery of novel compounds displaying potent anti-proliferative activities against colon cancers. Most of the compounds demonstrate potent cytotoxi...

The structures and one- and two-photon absorption properties of a series of phosphoryl substituted 3,5-bis(arylidene)piperid-4-ones bearing amino groups, nitro groups or fluorine atoms in the para-positions of the arene rings have been investigated. The measurable two-photon absorption cross sec...

A series of E,E-N-phosphorylalkylene-3,5-bis(arylidene)piperid-4-ones 7a–k was prepared via the condensation of aromatic aldehydes with ω-aminophosphonates 5a–c and 6a,b bearing piperidone or a protected piperidone moiety, respectively. The synthetic routes to the starting aminophosphonates 5...

(3E,5E)-3,5-Bis(benzylidene)-4-oxopiperidinium tetrafluoroborate [C19H18NO][BF4] (1), (3E,5E)-3,5-bis[4-(dimethylammonio)benzylidene]-4-oxopiperidinium bearing mixed tetrafluoroborate and bis(hexafluoro(μ-hydroxo)diborate) anions [C23H30N3O][B2F6OH]n[BF4]m·xH2O (2), and (3E,5E)-3,5-bis[4-(diet...

Reaction of 3,5-bis[(dimethylamino)methyl]phenyl iodide with 3,5-bis[(dimethylamino)methyl]phenylacetylene in diethylamine in the presence of bis(triphenylphosphine)palladium(II) dichloride (3.6 mol%) and copper(I) iodide (3.0 mol%) gave 1,2-(bis(3,5-bis[(dimethylamino)methyl]phenyl)acetylene (1...