The anticancer drug 2-chloro-2′-deoxyadenosine (CdA) belongs to the family of purine nucleoside analogs. CdA is exquisitely cytotoxic both to the dividing and to the non-dividing lymphocyte, which supports its use in lymphoproliferative disorders of low-grade malignancy. Indeed, the best clinic...

EHEB leukemic cells, which are derived from a patient suffering B-cell chronic lymphocytic leukemia (B-CLL), display intermediate sensitivity to the purine analogue 2-chloro-2′-deoxyadenosine (CdA). Because the mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase (ERK) ...

2-Chloro-2′-deoxyadenosine (Cladribine) chemotherapeutic drug has been studied experimentally in solid state by 35Cl NQR and NMR–NQR double resonance and theoretically by the Density Functional Theory. Fifteen resonance frequencies on 14N have been detected and assigned to particular nitrogen ...

To clarify the role of lipid rafts in 2-chloro-2′-deoxyadenosine (2CdA; Cladribine)-induced apoptosis, the effects of disruption of lipid rafts by methyl-β-cyclodextrin (MβCD) and filipin on 2CdA-induced apoptosis were investigated in four human acute lymphoblastic leukemia (ALL) cell lines c...

EHEB cells, a continuous cell line derived from a patient with B cell chronic lymphocytic leukemia (B-CLL), synthesized, when incubated with tritiated 2-chloro-2′-deoxyadenosine (CdA), labeled mono-, di-, and triphosphate ribonucleosides at a much higher rate than CdA deoxyribonucleotides. Furt...

The electrochemical oxidation process of 2-halogenoderivatives: 2-chloro-2′-deoxy- adenosine (2CldAdo), 2-bromo-2′-deoxyadenosine (2BrdAdo) and 2′-deoxyadenosine (2′dAdo) has been studied in aqueous buffered solutions by DPV and CV using a glassy-carbon electrode. All compounds investigated ...

A specific isocratic ion-pair HPLC method for the quantitation of mono-, di- and triphosphates of 2-chloro-2′-deoxyadenosine (CdA) in leukemic cells from patients is described. The method is based on an extraction of nucleotides from cells with a solution of perchloric acid containing triethyla...

The effects of 2-chloro-2′-deoxyadenosine (2CdA) on the activity of enzymes important for the metabolism of deoxyadenosine were studied in lysates prepared from human primary central nervous system (CNS) lymphomas and normal human lymphocytes. Strong inhibition (approximately 100%) of the phosp...

To assess the functions of the three human MutT-type enzymes, MTH1, MTH2, and NUDT5, mutation induction by an oxidized form of dGTP, 8-hydroxy-2′-deoxyguanosine 5′-triphosphate (8-OH-dGTP; 7,8-dihydro-8-oxo-2′-deoxyguanosine 5′-triphosphate), was examined using human 293T cells treated with ...

The reaction mechanism in the UV photochemistry of 2-chloro-2′-deoxyadenosine (Cladibrine) and 2-bromo-2′-deoxyadenosine in aqueous solution has been studied by laser photolysis at nanosecond time resolution. It is found that excitation at 266 nm wavelength produces heterolytic cleavage of the...

In the present study, the mechanism of antiplatelet activity of DK-002, a synthesized (6aS,cis)-9,10-Dimethoxy-7,11b-dihydro-indeno[2,1-c]chromene-3,6a-diol, was investigated. DK-002 inhibited the thrombin, collagen, and ADP-induced rat platelet aggregation in a concentration-dependent manner, w...

A procedure for the determination of nine phenoxy acid herbicides in water samples using gas chromatography in combination with mass spectrometric detection is presented. Analytes were concentrated from water samples using a solid-phase extraction (SPE) polymeric sorbent, functionalised with N-v...

A novel and potent series of ene-amides featuring azetidines has been developed as FabI inhibitors active against drug resistant Gram-positive pathogens particularly staphylococcal organisms. Most of the compounds from the series possessed excellent biochemical inhibition of Staphylococcus aureu...

The electrical-resistance-change method (ERCM) is a potential smart-sensing technique for carbon-fiber-reinforced plastic (CFRP) structures. However, a practical way to fabricate electrodes on CFRP structures, such as ink-jet printing with metal nano-inks, is necessary to reduce the time require...

The efficacy of dentin bonding system composed of a commercial or an experimental dentin cleanser, a dentin primer, and an intermediate resin was examined by measurement of the wall-to-wall polymerization contraction gap. Light-activated composites in a cylindrical dentin cavity were prepared in...

SummaryA toxic protein of Mr 22 000, called bolaffinine, has been purified from the mushroom, Boletus affinis Peck (Boletaceae), with a 0.65% yield using a procedure involving four steps: ammonium sulfate precipitation, two chromatographies on ion—exchange columns and gel filtration on Sephadex...

A medicinal chemistry program based on the small-molecule HCV NS5A inhibitor daclatasvir has led to the discovery of dimeric phenylthiazole compound 8, a novel and potent HCV NS5A inhibitor. The subsequent SAR studies and optimization revealed that the cycloalkyl amide derivatives 27a-29a exhibi...

This study was designed to characterize the role of vasopressin in impaired pial artery dilation to activators of the ATP sensitive K (KATP) and calcium sensitive K (Kca) channel following fluid percussion brain injury (FPI) in newborn pigs equipped with a closed cranial window. Topical vasopres...

To study vasopressin receptor-mediated endocytosis using electronmicroscopy methods and to develop avidin affinity columns for receptor purification, we synthesized and tested the biological properties of a biotinylated vasopressin (VP) analog [1-(2-mercapto) propionic acid] 8-[lysine-N6-biotin]...

The ability of vasopressin to elevate cytosolic Ca2+ in small cell lung cancer (SCLC) cells was investigated. Ten nanomolar vasopressin elevated the cytosolic Ca2+ in 6 of 8 SCLC cell lines that were loaded with Fura-2 AM. Using SCLC cell line NCI-H345, the effect of vasopressin was dose depende...