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Pyrazolones (3):
Recent article
Pyrazolones
Abstract
Synthesis of cyclopenta[b]pyrane derivatives via Achmatowicz oxidative cyclization of furanols followed by intramolecular Knoevenagel condensation of the β-ketoester arm is examined. The extent of diastereoselectivity was dependent on the nature of the chiral atom within the tethering carbon of the...
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PMID: 20856942
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PDF is available here.
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Abstract
We depict the synthesis and characterization of copper(II) and zinc(II) coordination compounds of 4-(3',4'-dimethoxybenzaldehydene)2-3-dimethyl-1-phenyl-3-pyrazolin-5-semicarbazone (1a), 4-(3',4'-dimethoxybenzaldehydene)2-3-dimethyl-1-phenyl-3-pyrazolin-5-thiosemicarbazone (1b), 4-(3'-hydroxy-4'-nit...
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PMID: 20363662
PDF is available here.
PDF is available here.
Abstract
About 66% (68/103) of the patients with an mPIM score (28 cases and 40 controls) had data on initial exposures. About 50% of the 28 cases and 18% of the 40 controls received an injection to treat fever during the first 96 hours after onset (Odds ratio [OR] = 7.0, 95% confidence interval [CI]: 1.8-28...
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PMID: 20104199
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PDF is available here.
Abstract
A reagent, 1-(4-isopropyl) phenyl-3-methyl-5-pyrazolone (PPMP) has been synthesized and used for high-performance liquid chromatography/electrospray ionization mass spectrometry (HPLC/ESI-MS) determination of pre-column labeled carbohydrates. Monosaccharides have been quantitatively converted into m...
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PMID: 20382576
PDF is available here.
PDF is available here.
Abstract
Arylhydrazonomalononitriles 1a,b react with phenylhydrazine to yield amidrazones 2a,b that cyclize to give 2-aryl-5-phenylhydrazono-2,5-dihydro-[1,2,4]-triazine-6-carbonitriles 5a,b upon reaction with dimethylformamide dimethylacetal (DMFDMA). Refluxing 5a,b in glacial acetic acid resulted in the fo...
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PMID: 20657480
PDF is available here.
PDF is available here.
Abstract
An efficient one-pot method to generate structurally diverse and medicinally interesting pyrazolone derivatives in good to excellent yields of 51-98% under microwave irradiation and solvent-free conditions has been developed.
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PMID: 20657501
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PDF is available here.
Abstract
Abstract
A new class of bis heterocycles-sulfone linked pyrazolyl oxadiazoles and thiadiazoles were developed from Z-styrylsulfonylacetic acid. The pyrazolyl thiadiazoles exhibited excellent antimicrobial activity whereas pyrazolyl oxadiazoles displayed good antioxidant activity.
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PMID: 19952447
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PDF is available here.
Abstract
We show the design and synthesis of new perfluorinated nitrosopyrazolone-based ligands and the original method employed for their complexation of erbium ions in the presence of the co-ligand perfluorotriphenylphosphine oxide; the resulting chelate is non-hygroscopic, solution processable and possess...
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PMID: 20448960
PDF is available here.
PDF is available here.
Carbohydrate Research (344)13 2009
Abstract
Synthesis of some novel 4-arylhydrazono-5-trifluoromethyl-2,4-dihydropyrazol-3-ones, their N- and N,O-bis- beta-D-glucosides is described. Antimicrobial evaluation of eight selected compounds against Aspergillus fumigatus RCMB 002008 (1), Penicillium italicum RCMB 001018 (1), Syncephalastrum racemos...
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PMID: 19570527
PDF is available here.
PDF is available here.
Abstract
A series of bidentate 1-(1-pyrazolylmethyl)-substituted NHC ligands (13a-c, 14a-c and 15a-c) were synthesised with substituents of varying steric bulk incorporated adjacent to the donor atoms. These ligands were coordinated to rhodium(I) to give a series of complexes of the general formula [Rh(L)(CO...
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PMID: 20449145
PDF is available here.
PDF is available here.
Abstract
The structural requirements relevant for protective efficacy against cisplatin-induced renal toxicity was studied for seven newly synthesized pyrazolone compounds. Since tetrahydroindazolonedicarboxylic acid (HIDA) has shown potential nephroprotective efficacy, our study involved HIDA derivatives wi...
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PMID: 19229375
PDF is available here.
PDF is available here.
Analytical Biochemistry (380)1 2008
Abstract
A new method for the determination of trace lead was developed by dispersive liquid-liquid microextraction preconcentration and graphite furnace atomic absorption spectrometry. In the proposed approach, 1-phenyl-3-methyl-4-benzoyl-5-pyrazolone (PMBP) was used as a chelating agent, and carbon tetrach...
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PMID: 18539126
PDF is available here.
PDF is available here.
Abstract
We performed a high-throughput in silico screen for small-molecular-weight compounds that bind the catalytic site of Shp2. We have identified the phenylhydrazonopyrazolone sulfonate PHPS1 as a potent and cell-permeable inhibitor, which is specific for Shp2 over the closely related tyrosine phosphata...
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PMID: 18480264
PDF is available here.
PDF is available here.
Abstract
Eight saccharides were derivatized using 1-(2-naphthyl)-3-methyl-5-pyrazolone (NMP) as pre-column derivatizing reagent, and separated on a reversed-phase Hypersil ODS 2 column (4.6 mm x 200 mm, 5 microm), by high performance liquid chromatography (HPLC) in conjunction with a gradient elution, detect...
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PMID: 18581853
PDF is available here.
PDF is available here.
Analytica Chimica Acta (609)1 2008
Abstract
A novel labeling reagent 1-(2-naphthyl)-3-methyl-5-pyrazolone (NMP) coupled with capillary electrophoresis (CE) with DAD detection for the determination of carbohydrates has been developed. The chromophore in the 1-phenyl-3-methyl-5-pyrazolone (PMP) reagent is replaced by naphthyl functional group,...
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PMID: 18243875
PDF is available here.
PDF is available here.
Abstract
Several 1,3-diaryl-5-(cyano-, aminocarbonyl- and ethoxycarbonyl-)-2-pyrazoline, pyrrolo[3,4-c]pyrazole-4,6-dione and 1,3,4,5-tetraaryl-2-pyrazoline derivatives were prepared by the reaction of nitrilimine with different dipolarophilic reagents. The new compounds were characterized using IR, (1)H-NMR...
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PMID: 18463603
PDF is available here.
PDF is available here.
Abstract
New Pd(II) and Pt(II) complexes [ML2] (HL=a substituted 2,5-dihydro-5-oxo-1H-pyrazolone-1-carbothioamide) have been synthesized by reacting K2MCl4 (M=Pd, Pt) or Pd(OAc)2 with beta-ketoester thiosemicarbazones. The structures of seven of these complexes were determined by X-ray diffraction. Although...
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PMID: 17689616
PDF is available here.
PDF is available here.
Abstract
Novel amino-pyrazolone, amino-isoxazolone and amino-pyrimidinone derivatives were prepared from ethyl 4-phenylsulfonyl-2-(2'-phenylsulfonylethyl)-2-cyanobutyrate (1), ethyl 4-arylsulfonyl-3-aryl-2-cyanobutyrate (7) and ethyl 4-arylmethylsulfonyl-3-aryl-2-cyanobutyrate (8). The lead molecules have be...
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PMID: 18057743
PDF is available here.
PDF is available here.
Abstract
We synthesized and evaluated various pyrazolone derivatives. Seven of 19 compounds showed inhibition of PrP-res accumulation and the remarkably active compound 13 showed an IC50 value of 3 nM in both ScN2a and F3 cell lines. Findings from studies on physicochemical and biochemical properties suggest...
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PMID: 17850126
PDF is available here.
PDF is available here.
Kidney International (72)6 2007
Abstract
We examine JNK signaling in the rat anti-glomerular basement membrane (GBM) disease model using CC-401, a specific JNK inhibitor. Animals were given CC-401, vehicle alone or no treatment starting before anti-GBM serum injection and continued treatment until killing. In acute disease, CC-401 blocked...
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PMID: 17597698
PDF is available here.
PDF is available here.
Abstract
Reactions of the cluster compound [Ru(3)(CO)(12)] with 5-trifluoromethyl-2,4-dihydropyrazol-3-one (HL(1)), 4-(2,4-dichlorophenylhydrazono)-5-trifluoromethyl-2,4-dihydropyrazol-3-one (H(2)L(2)), 4-(3-fluorophenylhydrazono)-5-trifluoromethyl-2,4-dihydropyrazol-3-one (H(2)L(3)), 4-(3-trifuoloromethyl-p...
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PMID: 17045838
PDF is available here.
PDF is available here.
Cancer Letters (249)2 2007
Abstract
We investigated the effect of Lgf-YL-9 on cytotoxicity and cell apoptosis in human epidermoid carcinoma drug-sensitive parental KB cells and multidrug resistant (MDR) KBv200 cells. Lgf-YL-9 exhibited potent cytotoxicity not only to KB cells but also to KBv200 cells, and the IC(50) were 3.81 and 3.45...
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PMID: 17055640
PDF is available here.
PDF is available here.
Abstract
We disclosed a structure-based kinase inhibitor design strategy which led to the identification of a new class of VEGFR-2/KDR kinase inhibitors bearing heterocyclic substituted pyrazolones as the core template. Instability in a rat S9 preparation and poor iv PK profiles for most of these inhibitors...
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PMID: 17239587
PDF is available here.
PDF is available here.
Abstract
During a sport competition event in Taiwan, one urine specimen was found positive for both methamphetamine (2688 ng/mL) and amphetamine (462 ng/mL). The specimen donor claimed that she had taken Gewolen (a nonprescription drug manufactured in Taiwan) for treating abdominal pain and the medication wa...
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PMID: 17316255
PDF is available here.
PDF is available here.
Abstract
A series of novel 3(5)-aryl/ferrocenyl-5(3)-phenothiazinylpyrazoles and pyrazolines were obtained by substituent-dependent regioselective condensation of the corresponding (E)-3-(2-alkyl-10H-phenothiazin-3-yl)-1-aryl/ferrocenylprop-2-en-1-one with hydrazine or methylhydrazine in acetic acid. The dif...
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PMID: 17102884
PDF is available here.
PDF is available here.
Abstract
We synthesized various 3-methyl-1-phenyl-5-pyrazolone (edaravone) derivatives and evaluated their oxidation potential and hydroxyl radical scavenging activity. It was found 3-methyl-1-(pyridin-2-yl)-5-pyrazolone had a much higher ability to scavenge the radical than did edaravone itself. Its efficie...
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PMID: 16997555
PDF is available here.
PDF is available here.
Abstract
The synthesis of 5-indolylpyrazol-3-one, 4-indolylpyrazol-3-one and 4-indolyl-pyridazin-3,6-dione is reported. Their Chk1 inhibitory properties have been evaluated and their in vitro antiproliferative activities toward three tumor cell lines: murine leukemia L1210, human colon carcinoma HT29 and HCT1...
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PMID: 16996169
PDF is available here.
PDF is available here.
Inorganic Chemistry (45)18 2006
Abstract
The reaction of [ReX(CO)5] with thiosemicarbazones H2L(R) derived from beta-keto esters (X = Cl, Br; R = Me, Ph) allowed the isolation of cyclic trimeric complexes [Re3(pyz(R))3(CO)9], where pyz(R) is the pyrazolonate corresponding to the thiosemicarbazone. Electron spray ionization Fourier transfor...
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PMID: 16933934
PDF is available here.
PDF is available here.
Abstract
Abstract
We have described the synthesis of tridentate pyrazolyl ligand frameworks for coordination to the fac-[*M(CO)(3)](+) metal fragment (*M=(186/188)Re or (99m)Tc). These ligands impart a degree of kinetic inertness on the metal center, warranting their study in biological systems. We herein report in v...
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PMID: 16843837
PDF is available here.
PDF is available here.
Abstract
Synthetic hybridization of two privileged drug scaffolds, pyrazolone on the one hand and pyrimidine nucleoside on the other, resulted in the generation of two novel 5-substituted pyrimidine nucleosides with potent in vitro antiviral activity against two representative orthopoxviruses, vaccinia virus...
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PMID: 16603351
PDF is available here.
PDF is available here.
Abstract
Structural analysis of the essential binding elements of the oxindole-based kinase inhibitor (1) led to the identification of a novel class of heterocyclic-substituted pyrazolones. Knoevenagel condensation of a variety of activated methylene nucleophiles with indole or pyrrole carboxaldehydes provid...
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PMID: 16460933
PDF is available here.
PDF is available here.
Abstract
We report the syntheses and biological evaluation of novel inhibitors based on the estrone or estradiol template. These have been investigated by modification at the 6, 16 or 17 positions or combinations of these in order to gain information about structure-activity relationships by probing differen...
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PMID: 16480268
PDF is available here.
PDF is available here.
Abstract
The risk of agranulocytosis associated with the use of pyrazolone drugs at therapeutical doses and for short periods of time has been considered to be very low. However, little or no attention at all has been devoted to the possible hindrance of neutrophil burst and scavenging of neutrophil-generate...
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PMID: 16458194
PDF is available here.
PDF is available here.
Abstract
A series of conformationally constrained bicyclic derivatives derived from SR141716 was prepared and evaluated as hCB(1)-R antagonists and inverse agonists. Optimization of the structure-activity relationships around the 2,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one derivative 2a led to the identificat...
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PMID: 16263283
PDF is available here.
PDF is available here.
Abstract
A series of 13 anthrapyrazole compounds that are analogues of piroxantrone and losoxantrone were synthesized, and their cell growth inhibitory effects, DNA binding, topoisomerase IIalpha mediated (EC 5.99.1.3) cleavage of DNA, and inhibition of DNA topoisomerase IIalpha decatenation catalytic activi...
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PMID: 16859314
PDF is available here.
PDF is available here.
Abstract
New compounds, structurally related to the potent protein kinase C inhibitor staurosporine, with a bisindolylpyrazolone framework and substituted on the pyrazolone nitrogens with N,N-dialkylaminoalkyl side chain, were synthesized and evaluated for growth-inhibitory properties in several human cell l...
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PMID: 16263294
PDF is available here.
PDF is available here.
European Journal of Pharmacology (528)1-3 2005
Abstract
We propose that EK-6136 is an active HTS hit as a Cdc25B inhibitor with antiproliferative activity, and can be used for the design of more potent and selective antiproliferative agents....
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PMID: 16324698
PDF is available here.
PDF is available here.
Abstract
Inorganic Chemistry (44)24 2005
Abstract
Three pyrazolone-based ligands, namely 1-phenyl-3-methyl-4-(1-naphthoyl)-5-pyrazolone (HL1), 1-phenyl-3-methyl-4-(4-dimethylaminobenzoyl)-5-pyrazolone (HL2), and 1-phenyl-3-methyl-4-(4-cyanobenzoyl)-5-pyrazolone (HL3), were synthesized by introducing electron-poor or electron-rich aryl substituents...
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PMID: 16296848
PDF is available here.
PDF is available here.
Abstract
Inorganic Chemistry (44)22 2005
Abstract
New [CpM(Q)Cl] complexes (M = Rh or Ir, Cp = pentamethylcyclopentadienyl, HQ = 1-phenyl-3-methyl-4R(C=O)-pyrazol-5-one in general, in detail HQ(Me), R = CH(3); HQ(Et), R = CH(2)CH(3); HQ(Piv), R = CH(2)-C(CH(3))(3); HQ(Bn), R = CH(2)-(C(6)H(5)); HQ(S), R = CH-(C(6)H(5))(2)) have been synthesized fro...
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PMID: 16241143
PDF is available here.
PDF is available here.
Abstract
A new photochromic compound 1,3-diphenyl-4-(4'-fluro)benzal-5-pyrazolone-4-ethyl thiosemicarbazone (DP4FBP-ETSC) was synthesized by direct condensation of 1,3-diphenyl-5-pyrazolone with N4-ethyl thiosemicarbazide. The product was characterized by elemental analysis, IR and 1H NMR spectra. The photoc...
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PMID: 16043052
PDF is available here.
PDF is available here.
Abstract
In non-aqueous solvent, a new amino-acid schiff base, 1-phenyl-3-methyl-4-benzoyl pyrazolone-5-beta-alanine (HL) was synthesized by a reaction of beta-alanine with benzoylpyrazolone, and its ten rare earth complexes were obtained from refluxing a solution of schiff base and rare earth nitrates. On t...
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PMID: 16379296
PDF is available here.
PDF is available here.
Abstract
Several primary murine and human B lymphomas and cell lines were found to constitutively express high levels of the activated form of c-jun N-terminal kinase (JNK), a member of the mitogen-activated protein (MAP) kinase family. Proliferation of murine B lymphomas CH31, CH12.Lx, BKS-2, and WEHI-231 a...
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PMID: 15890690
PDF is available here.
PDF is available here.
Abstract
We identified a pyrazolone that reversibly blocked the activation of phagocyte oxidase (phox) in human neutrophils in response to tumor necrosis factor (TNF) or formylated peptide. The pyrazolone spared activation of phox by phorbol ester or bacteria, bacterial killing, TNF-induced granule exocytosi...
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PMID: 16043520
PDF is available here.
PDF is available here.
Abstract
4-Aryl-5-pyrimidyl based cytokine synthesis inhibitors that contain a novel monocyclic, pyrazolone heterocyclic core are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-alpha production. One of the compounds (6e) was found to be efficacious in the rat iodoac...
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PMID: 15837310
PDF is available here.
PDF is available here.
Abstract
A new Schiff base containing sulphur, 1-phenyl-3-methyl-4-(alpha-furoyl) pyrazolone-5-thiosemicarbazone (HL) and its Zn(II), Cd(II) and Co(II) complexes have been synthesized. On the basis of elemental analysis and molar conductance, the general formulae of the complexes, [ZnL2] x 1.5H2O, [CdL2] x C...
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PMID: 15852859
PDF is available here.
PDF is available here.
Terapevticheskii arkhiv (77)2 2005
Abstract
Comparative evaluation was made of clinical efficacy of combined therapy reaferon + iodantipirin and monotherapy with reaferon in 100 patients with moderate activity CHB and C. CONCLUSION: Conventional scheme with reaferon turned out less effective than the above combination therapy....
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PMID: 15807459
PDF is available here.
PDF is available here.
Revista Medico-Chirurgicala (109)2 2005
Abstract
We carried out our determinations at 362 nm, where the absorbency of famotidine - picrolonic acid complex is maximal, and we have established the optimal reaction conditions. This method was successfully applied for famotidine assay from pharmaceutical dosage forms....
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PMID: 16607813
PDF is available here.
PDF is available here.
Abstract
One of the 14 different drugs known to be metabolized to methamphetamine and/or amphetamine is famprofazone, a component in the multi-ingredient formulation Gewodin. Because of its conversion to methamphetamine and amphetamine, which can result in positive drug-testing results, the excretion pattern...
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PMID: 15516292
PDF is available here.
PDF is available here.
Transplantation (78)3 2004
Abstract
JNK inhibition decreases hepatic necrosis and apoptosis after OLT, suggesting that JNK activation promotes cell death by both pathways. Inhibition of JNK may be a new therapeutic strategy to prevent liver injury after transplantation....
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PMID: 15316358
PDF is available here.
PDF is available here.
Abstract
Novel substituted [5,5]-bicyclic pyrzazolones are presented as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production. Many of these compounds show low nanomolar activity against lipopolysaccaride (LPS)-induced TNF-alpha production in THP-1 cells. This class of molecules was co-crystallize...
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PMID: 15261284
PDF is available here.
PDF is available here.
Abstract
These results demonstrate that TELIN is a specific potent catalytic blocker of telomerase,and is considered to be a valuable substance for medical treatment of cancer and related diseases....
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PMID: 15303281
PDF is available here.
PDF is available here.
Journal of Biotechnology (110)1 2004
Abstract
Nostocine A (1) is an extracellular cytotoxic violet pigment produced by the freshwater cyanobacterium, Nostoc spongiaeforme TISTR 8169. Treatment with 1 was found to accelerate the generation of reactive oxygen species (ROS) in the green alga, Chlamydomonas reinhardtii, in the light. In vitro analy...
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PMID: 15099903
PDF is available here.
PDF is available here.
Abstract
In search of a novel chemotype of K(ATP) channel openers a series of tricyclic dihydropyridopyrazolones and dihydropyridoisoxazolones was synthesized. It was found that cyclopentanone in the left hand portion of the molecule was 4-fold more potent than cyclohexanone. Introduction of gem-dimethyl gro...
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PMID: 15051058
PDF is available here.
PDF is available here.
Abstract
An approach was developed to screening organic compounds for putative activity of redox mediators of oxidoreductases, including laccases and peroxidases, applicable for xenobiotic degradation. The study was carried out with a homogenous laccase preparation from the basidiomycete Trametes hirsuta and...
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PMID: 15125193
PDF is available here.
PDF is available here.
Abstract
There are a several drugs that lead to the production of methamphetamine and/or amphetamine in the body which are subsequently excreted in the urine. These drugs raise obvious concerns when interpreting positive amphetamine drug testing results. Famprofazone is an analgesic found in a multi-ingredie...
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PMID: 14607003
PDF is available here.
PDF is available here.
Abstract
3-phenyl-4-arylazo-5-pyrazolones (I-IV) have been synthesized and characterized by elemental, infrared (IR), ultraviolet and visible spectra (UV-Vis), proton nuclear magnetic resonance (1H NMR) and Mass spectra. It has been proved that these compounds exhibit a keto-enol tautomerism in solution. The...
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PMID: 12963440
PDF is available here.
PDF is available here.