Title:Microwave Assisted One-Pot Synthesis of Novel Trifluoromethyl Coumarin Thiosemicarbazones and their Antifungal Activities. VOLUME: 3 ISSUE: 1. Author(s):Guoyu Yang, Cuilian Xu, Mingqin Zhao, Caixia Wang, Sufang Fan, Puhui Xie and Xin Li. Affiliation:College of Sciences, Henan Agricultural University, Zhengzhou 450002, P. R. of China.. Keywords:Antifungal activity, microwave synthesis, one-pot synthesis, solvent-free, trifluoromethyl coumarin thiosemicarbazones.. Abstract:Some new trifluoromethyl coumarin thiosemicarbazones 3a-3m were synthesized by condensation reaction of thiosemicarbazides and 3-trifluoroacetyl coumarins which was from recyclization of ethyl 2-hydroxy-2-(trifluoromethyl)-2H-chromene-3-carboxylates under microwave assisted and solvent-free conditions. The structure of the synthesized compounds were characterized by IR, 1H NMR, 13C NMR, HRMS and X-ray, and their antifungal activity was evaluated. Most of them exhibited potent antifungal activity by comparison with the ...

Pancreatic cancer is an aggressive disease, with a poor response to the currently available treatments, including the standard gemcitabine (Jemal et al., 2009). To this end, we examined a new class of thiosemicarbazones that are designed to target the crucial nutrient iron (Richardson et al., 2009). Thiosemicarbazones have been found to have potent and selective activity against a range of different tumors (Yuan et al., 2004; Kalinowski and Richardson, 2005; Whitnall et al., 2006). In fact, these agents were also demonstrated to overcome chemoresistance (Whitnall et al., 2006), which is an appreciable problem in the treatment of pancreatic cancer (Custodio et al., 2009). However, the efficacy of these novel thiosemicarbazones against pancreatic cancer has not been assessed previously.. One of the first indicators that thiosemicarbazones and other iron chelators may be a suitable strategy for the treatment of pancreatic cancer was the finding that they up-regulate the growth and metastasis ...

TY - JOUR. T1 - Zinc(II). T2 - Thiosemicarbazone complexes are localized to the Lysosomal compartment where they transmetallate with Copper Ions to induce Cytotoxicity. AU - Stacy, Alexandra E. AU - Palanimuthu, Duraippandi. AU - Bernhardt, Paul V. AU - Kalinowski, Danuta. AU - Jansson, Patric J. AU - Richardson, Des. N1 - Imported on 16 May 2017 - DigiTool details were: publisher = American Chemical Society, 2016. Volume no. (773r) = 59; Issue no. (773s) = 10; Parent title (773t) = Journal of Medicinal Chemistry. ISSNs: 0022-2623; PY - 2016. Y1 - 2016. N2 - As the di-2-pyridylketone thiosemicarbazone (DpT) and 2-acetylpyridine thiosemicarbazone (ApT) series show potent antitumor activity in vitro and in vivo, we synthesized their fluorescent zinc(II) complexes to assess their intracellular distribution. The Zn(II) complexes generally showed significantly greater cytotoxicity than the thiosemicarbazones alone in several tumor cell-types. Notably, specific structure-activity relationships ...

TY - JOUR. T1 - Copper complexes of bis(thiosemicarbazones). T2 - From chemotherapeutics to diagnostic and therapeutic radiopharmaceuticals. AU - Paterson, Brett M.. AU - Donnelly, Paul S.. PY - 2011/5. Y1 - 2011/5. N2 - The molecules known as bis(thiosemicarbazones) derived from 1,2-diones can act as tetradentate ligands for Cu(ii), forming stable, neutral complexes. As a family, these complexes possess fascinating biological activity. This critical review presents an historical perspective of their progression from potential chemotherapeutics through to more recent applications in nuclear medicine. Methods of synthesis are presented followed by studies focusing on their potential application as anti-cancer agents and more recent investigations into their potential as therapeutics for Alzheimers disease. The Cu(ii) complexes are of sufficient stability to be used to coordinate copper radioisotopes for application in diagnostic and therapeutic radiopharmaceuticals. Detailed understanding of the ...

Our data demonstrate that BAF can impair HSV-1 infection in a manner regulated by localization and/or phosphorylation, thus paralleling how BAFs anti-poxviral activity is modulated. In vivo toxicity was assessed on skin tissues of mice after mice treatment with whole latex and processing for histology. The results of this work are in agreement with previous randomized, double-blind versus placebo multicentre studies examining the effects of 72 mg of PAC-standardized cranberry. HE staining also showed that in 5mg/kg CV-N and 10mg/kg CV-N treated groups, the brain cells did not show visible changes, except for a slight inflammation. The Bifidobacterium adolescentis SPM 0214 used in this study through the screening of 23 Bifidobacterium spp. We propose that upon HSV-1 stimulation, RIP3 promotes the recruitment of TBK1 to STING, which leads to TBK1-mediated IRF3 activation and subsequent type I IFN secretion. A concentration of 50μM TF3 and above was sufficient to inhibit >99% of the production of ...

Other names: 2-Formyl-1-methylpyrrole; N-Methyl-2-formylpyrrole; 1-Methyl-2-formylpyrrole; N-Methylpyrrole-2-carboxaldehyde; 1-Methyl-1H-pyrrole-2-carboxaldehyde; 1-Methylpyrrole-2-carboxaldehyde; Pyrrole-2-carboxaldehyde, 1-methyl-; N-Methylpyrrole-2-carbaldehyde; 1-Methyl-1H-pyrrole-2-carbaldehyde; 1-Methyl-2-pyrrolaldehyde; 1-Methyl-2-pyrrolecarboxaldehyde; 1-Methylpyrrole-2-carbaldehyde; 1-Methylpyrrole-2-carboxyaldehyde; N-Methylpyrrole-2-carboxy aldehyde; NSC 72386; 1-methylformylpyrrole ...

The antineoplastic activity of α‐N‐heterocyclic thiosemicarbazones was discovered several decades ago. Currently the most promising drug candidate of this class of compounds is Triapine (3‐aminopyridine‐2‐carboxaldehyde thiosemicarbazone, 3‐AP), which entered several phase I and II clinical trials as an antitumor agent. We discovered that Triapine possesses intrinsic fluorescence properties. This enabled us to monitor for the first time the uptake and intracellular distribution of an α‐N‐heterocyclic thiosemicarbazone in living human cancer cells by fluorescence microscopy. In addition we synthesized the first zinc(II) complex [Zn(Triapine)Cl2]•HCl of Triapine, which shows fluorescence as well, compared its cytotoxicity in human cancer cells with that of the parental compound and studied the influence of metal complexation on intracellular distribution.. Triapine and its zinc complex were characterized spectroscopically. The UV‐Vis spectrum of Triapine in water shows a ...

(R)-(+)-2,2-Dimethyl-1,3-dioxolane-4-carboxaldehyde 15186-48-8 NMR spectrum, (R)-(+)-2,2-Dimethyl-1,3-dioxolane-4-carboxaldehyde H-NMR spectral analysis, (R)-(+)-2,2-Dimethyl-1,3-dioxolane-4-carboxaldehyde C-NMR spectral analysis ect.

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TY - JOUR. T1 - Studies on the mechanism of hypoxic selectivity in copper bis(thiosemicarbazone) radiopharmaceuticals. AU - Maurer, Richard I.. AU - Blower, Philip J.. AU - Dilworth, Jonathan R.. AU - Reynolds, Christopher A.. AU - Zheng, Yifan. AU - Mullen, Gregory E.D.. PY - 2002/3/1. Y1 - 2002/3/1. N2 - Copper diacetyl-bis(N4-methylthiosemicarbazone), Cu(II)ATSM, is a promising agent for imaging hypoxic tissue. Here we present results that provide insight into the chemical and electronic properties underlying previously observed structure-activity relationships. Density functional theory (DFT) calculations on the electronic structures and molecular orbitals of a series of 13 Cu(II)bis(thiosemicarbazone) analogues with different alkylation patterns and with fixed geometries based on the known structure of Cu(II)PTSM showed that the LUMO and the next lowest orbital were very close in energy, and their energy order was strikingly dependent on the ligand alkylation pattern in a way that ...

Breast cancer is the first cause of cancer death in women. Many patients are resistant to current therapies, and even those were sensitive at first may eventually become resistant later. Thiosemicarbazones (TSCs) are synthetic compounds that exhibit several pharmacological activities. In this study, we investigated the potential anti-tumor activity of a set of N4 -arylsubstituted TSCs (N4 -TSCs) on human breast cancer cell lines. Studies on the effect of N4 -TSCs (T1, T2 and T3) were carried on MCF-7, MDA-MB 231 and BT 474 cell lines which differ in their expression of ER, PR and Her2/neu. Non-transformed MCF-10A breast cell line were used as normal cells. Action of N4 -TSCs were evaluated by proliferation assay, quantification of apoptosis and cell cycle analysis. Modulation of clonogenic efficiency and migratory capacity by N4 -TSCs were also evaluated. We further investigated the effects of N4 -TSCs on ROS level and Ribonucleotide Reductase (RR) activity. We analyzed the action of these compounds on

C,H,N analyses suggest that H3FPT and H4FPT form 2:1 ligand-to-metal complexes with nickel(II), in which one of the ligands is neutral and the other anionic, similar to an iron(III) complex of 2-acetylpyridine thiosemicarbazone obtained by us in a previous work11. The molar conductivity measurements indicate that both complexes are 1:1 electrolytes, consistent with the presence of the perchlorate bands in the infrared spectrum (vide infra). The complex [Ni(H4FPT)(4FPT)]ClO4 is diamagnetic, suggesting square planar geometry but in the case of [Ni(H3FPT)(3FPT)]ClO4 the measured magnetic susceptibility of 3.0 BM is close to the theoretical value of 2.83 BM of tetrahedral arrangement. The 1H-NMR spectrum of the former shows a peak at d = 11.398, assigned to the protonated ligand s N(2 )-H hydrogen bonded to DMSO9. Also, the signal at d = 7.992 in the spectrum of H4FPT, assigned to the formyl proton, is shifted to higher frequency (d = 7.998) upon coordination of the azomethine nitrogen N(1 ). H3APT ...

In this study, tumor sub-volumes were defined based on a DPBC strategy of FDG and 64Cu-ATSM PET, and the overlap between these sub-volumes was analyzed.. Two cut-off values for FDG uptake were explored, and 64Cu-ATSM uptake was analyzed by sub-volumes based on two different time-points for image acquisition. We observed an overlap between all 64Cu-ATSM and FDG sub-volumes. However, the degree of overlap varied between cases.. Our results showed that a fairly large part of the hypoxic sub-volume as defined by 64Cu-ATSM was not included in a boost volume based on FDG uptake with the chosen thresholds. However, the hypoxic sub-volume did not encompass the FDG uptake either, and it therefore seems attractive to include both tracers in RT planning considering their association to treatment outcome and prognosis.. The Cu24 sub-volume was predominantly included in the BTV consisting of FDG (FDG40 or FDG50) and Cu3. This result suggests that the temporal variations of 64Cu-ATSM uptake might be taken ...

Thiosemicarbazone ligand 4Hbatsc = 4-hydroxybenzaldehyde-thiosemicarbazone and its silver(I) complex [Ag(PPh3)3(4Hbatsc)]NO3 were synthesized and characterized by elemental analysis (CHN), FT-IR spectroscopy, and single-crystal X-ray diffraction. The triclinic unit cell of 4H-ba-tsc (space group P-1) contains two independent molecules. Each of the two independent molecules is almost planar, with the sulfur atom (S1/S2) and the hydrazine nitrogen atom (N6/N4) in the E position concerning the C3-N5/C4-N4. The title complex is a triclinic P-1 mononuclear complex with the silver(I) ion coordinated in a distorted tetrahedral geometry by one S atom of 4H-ba-tsc and three P atoms of three PPh3. The complex involves the 4H-ba-tsc thiosemicarbazone ligand in an S monodentate binding mode. Besides, the thermal behavior of the complex was studied using thermogravimetry in order to evaluate its thermal stability and thermal decomposition pathway. Finally, nanoparticles of the complex were prepared in an ultrasonic

4-Aminopyridine-2,6-Dicarboxylic Acid (CAS 2683-49-0) Market Research Report 2018 aims at providing comprehensive data on 4-aminopyridine-2,6-dicarboxylic

A family of heterocyclic thiosemicarbazone dyes (3a-f and 4) containing furyl groups was synthesized in good yields, characterized and their response in acetonitrile in the presence of selected anions was studied. Acetonitrile solutions of 3a-f and 4 showed absorption bands in the 335-396 nm range which are modulated by the electron donor or acceptor strength of the heterocyclic systems appended to the thiosemicarbazone moiety. Fluoride, chloride, bromide, iodide, dihydrogen phosphate, hydrogen sulphate, nitrate, acetate and cyanide anions were used in recognition studies. From these anions, only sensing features were seen for fluoride, cyanide, acetate and dihydrogen phosphate. Two clearly different chromo-fluorogenic behaviours were observed: (i) a small shift of the absorption band due to the coordination of the anions with the thiourea protons and (ii) the appearance of a new red shifted band due to deprotonation. For the latter effect, a change in the colour of solution from pale yellow to ...

The thiosemicarbazone derivative of 9,10-phenanthrenequinone, 1, and its metal complexes were synthesized. The X-ray crystal structure for 1 confirms the presence of the E tautomeric arrangement in this compound. Its copper complex shows 1:1 stoichiometry while nickel and cobalt compounds show 1:2 stoichiometry. The X-ray crystal structure of the nickel complex indicates two tridentate ligands coordinating in the thiolato form yielding an octahedral geometry for the mer isomer. The copper complex exhibits maximum antiproliferative activity against human breast cancer cell-line, T47D probably due to inhibition of steroid binding to the cognative receptor or by preventing dimerization of the estrogen receptor.

A range of new carboxylate functionalised bis(thiosemicarbazone) ligands and their Cu(II) complexes have been prepared, fully characterised and radiolabeled in high yield with both (64)Cu and (99m)Tc. Conjugation to a bombesin derivative was achieved using standard solid phase synthetic

New N(4)-methylthiosemicarbazone derivatives: Synthesis, characterization, structural properties, DNA interactions and antiproliferative activity

TY - JOUR. T1 - Synthesis and evaluation of folate-bis(thiosemicarbazone and folate-cyclam conjugates for possible use as folate-receptor-targeted copper radiopharmaceuticals. AU - Ke, C. Y.. AU - Mathias, C. J.. AU - Yang, Z. F.. AU - Luo, J.. AU - Low, P. S.. AU - Waters, D. J.. AU - Green, M. A.. PY - 1999/1/1. Y1 - 1999/1/1. KW - Copper-64. KW - Copper-67. KW - Folate receptor. KW - Tumor targeting. UR - http://www.scopus.com/inward/record.url?scp=0032773127&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=0032773127&partnerID=8YFLogxK. M3 - Article. AN - SCOPUS:0032773127. VL - 42. SP - S821-S823. JO - Journal of Labelled Compounds and Radiopharmaceuticals. JF - Journal of Labelled Compounds and Radiopharmaceuticals. SN - 0362-4803. IS - SUPPL. 1. ER - ...

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PubMed Central Canada (PMC Canada) provides free access to a stable and permanent online digital archive of full-text, peer-reviewed health and life sciences research publications. It builds on PubMed Central (PMC), the U.S. National Institutes of Health (NIH) free digital archive of biomedical and life sciences journal literature and is a member of the broader PMC International (PMCI) network of e-repositories.

The organoruthenium complex [(η6-p-cym)Ru(η1-S-TSC)Cl2], (1) and (2-acetyl-5-methyl-thiophene thiosemicarbazone) TSC ligand were investigated in vitro fo...

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Coordination chemistry. Assuming a > p: (i) Write the electronic configuration of d 4 ion. The IC50 values for the two complexes are > 200 and 8.96 μM for [{Ru(p-cymene)Cl}2(L158)]Cl2 and [{Ru(C6H5C3H6COOH)Cl}2(L158)]Cl2, respectively. Use of an excess of lanthanide oxide should be avoided since reactions of the following type may take place [38]. Complexes 141 and 142 with piperonal thiosemicarbazones216 and 155 and 156 with anthraldehyde thiosemicarbazones217 were tested for antiproliferative activity in two human cancer cell lines, HCT116 (colon) and Caco2 (epithelial colorectal), as well as in a nontumorigenic (CCD-18Co) cell line. NH 2 - NH 3 + hydrazinium. Explanations would be wonderful! The other classes are derivatives of ethanolamine, alkylamine, piperazine, and others (primarily tricyclic and tetracyclic compounds related to phenothiazines, tricyclic antidepressants, as well as the cyproheptadine-phenindamine family), Ethylenediamine, because it contains two amine groups, is a widely ...

Over the past years cancer statistics have continued to rise to the point that the World Health Organization said that in 2005 cancer was leading cause of death worldwide. Years of research have resulted in many new ...

PubMed Central Canada (PMC Canada) provides free access to a stable and permanent online digital archive of full-text, peer-reviewed health and life sciences research publications. It builds on PubMed Central (PMC), the U.S. National Institutes of Health (NIH) free digital archive of biomedical and life sciences journal literature and is a member of the broader PMC International (PMCI) network of e-repositories.

The trapping mechanisms of the PET hypoxia imaging agent copper(II)-diacetyl-bis(N4-methylthiosemicarbazone) (64Cu(ATSM)) remain unresolved, although its reduction prior to dissociation may be mediated by intracellular thiols. Glutathione (GSH) is the most abundant intracellular thiol, and its redox status changes in cancer cells and ischaemic myocardium (two prime applications for 64Cu(ATSM) PET). We therefore investigated whether modification of intracellular GSH content affects the hypoxia selectivity of 64Cu(ATSM). Isolated rat hearts (n = five per group) were perfused with aerobic buffer (equilibrated with 95%O2/5%CO2) for 15 min, then hypoxic buffer (95%N2/5%CO2) for 20 min. Cardiac glutathione was depleted by buthionine sulphoximine (BSO, 4 mmol/kg/ 48 h intraperitoneal), or augmented by N-acetyl cysteine (NAC, 4 mmol/L) in the perfusion buffer. Cardiac 64Cu retention from three 2-MBq bolus injections of 64Cu(ATSM) before and during hypoxia was then monitored by NaI detectors. Cardiac GSH content

Tumor hypoxia (low tissue oxygenation) is an adverse condition of the solid tumor environment, associated with malignant progression, radiotherapy resistance, and poor prognosis. One method to detect tumor hypoxia is by positron emission tomography (PET) with the tracer [64Cu][Cu-diacetyl-bis(N(4)-methylthiosemicarbazone)] ([64Cu][Cu(ATSM)]), as demonstrated in both preclinical and clinical studies. In addition, emerging studies suggest using [64Cu][Cu(ATSM)] for molecular radiotherapy, mainly due to the release of therapeutic Auger electrons from copper-64, making [64Cu][Cu(ATSM)] a

Abstract:. Ask for Free Sample @ WMR- https://westernmarketresearch.com/sample-report/1144642/Europe Benzo[b]thiophene-2-carboxaldehyd#sample. The Europe Benzo[b]thiophene-2-carboxaldehyde market size is $XX million USD in 2018 with XX CAGR from 2014 to 2018, and it is expected to reach $XX million USD by the end of 2024 with a CAGR of XX% from 2019 to 2024.. Ask for Free Sample-Inquiry and Discount @WMR- https://westernmarketresearch.com/market-report/1144642/Europe Benzo[b]thiophene-2-carboxaldehyd#inquiry. This report is an essential reference for who looks for detailed information on Europe Benzo[b]thiophene-2-carboxaldehyde market. The report covers data on Europe markets including historical and future trends for supply, market size, prices, trading, competition and value chain as well as Europe major vendors°Ø information. In addition to the data part, the report also provides overview of Benzo[b]thiophene-2-carboxaldehyde market, including classification, application, manufacturing ...

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TY - JOUR. T1 - Regional myocardial perfusion assessed with generator-produced copper- 62-PTSM and PET. AU - Herrero, Pilar. AU - Hartman, Judy J.. AU - Green, Mark A.. AU - Anderson, Carolyn J.. AU - Welch, Michael J.. AU - Markham, Joanne. AU - Bergmann, Steven R.. PY - 1996/8/1. Y1 - 1996/8/1. N2 - We have previously demonstrated that myocardial perfusion can be estimated accurately in experimental animals with the generator-produced positron-emitting tracer, 62Cu-pyruvaldehyde bis (N4-methylthio- semicarbazone)(62Cu-PTSM) and PET. This study evaluated the feasibility of quantifying regional myocardial blood flow using 62Cu-PTSM and PET in human subjects. Methods: Regional perfusion was estimated using a previously described and validated two-compartment model from dynamic PET scans obtained after an intravenous bolus of 62Cu-PTSM in 10 healthy volunteers and in 6 patients with coronary artery disease at rest; and in 9 of the volunteers and 4 of the patients after administration of ...

Copper bis(4-ethyl-3-thiosemicarbazonato) acenaphthenequinone (1) and copper bis(4-methyl-3-thiosemicarbazonato) acenaphthenequinone (2) are synthesized and characterized in solution, in the solid state, and radiolabeled. Serum-protein binding radioassays show good stability in solution and about 25 % binding to protein over 1 h, which is comparable with the hypoxia selective tracer [(64)Cu(ATSM)]. Cyclic voltammetry shows fast and reversible reduction at redox potentials similar to the values known for hypoxia-selective copper compounds. However, despite this, complex 1 does not show any hypoxic-selective uptake in HeLa cells over 1-h standard assays. Possible reasons for this are studied by using the intrinsic fluorescence of the Cu(II) complexes to determine the cellular distributions and uptake mechanism by confocal microscopy. The complexes are found to bind to the external cell membrane and disperse evenly in the cytoplasm only after a very slow cell internalization (|1 h). No significant changes

The interaction between isatin-β-thiosemicarbazone (IBT) and calf thymus DNA (CT-DNA) was investigated in physiological buffer (pH 7.4) using Neutral Red (NR) dye as a spectral probe by UV-Vis absorption and fluorescence spectroscopy, as well as viscosity measurements. The IBT is stabilized by intercalation in the DNA ( K [IBT -DNA] =1.03×105 M−1), and displaces the NR dye from the NR-DNA complex. The binding constants Kf and number of binding sites (n≈1) of IBT with DNA were obtained by fluorescence quenching method at different temperatures. Furthermore, the enthalpy and entropy of the reaction between IBT and CT-DNA showed that the reaction is enthalpy-favored and entropy-disfavored. The changes in the base stacking of CT-DNA upon the binding of IBT are reflected in the circular dichroic (CD) spectral studies. The viscosity increase of CT-DNA solution is another evidence to indicate that, IBT is able to be intercalated in the DNA base pairs.

The treatment of leishmaniasis with pentavalent antimonials is problematic because of their toxicity. Investigations of potentially active molecules are important to discover less toxic drugs that are viable economic alternatives for the treatment of leishmaniasis. Thiosemicarbazones are a group of molecules that are known for their wide versatility and biological activity. In the present study, we examined the antileishmania activity, mechanism of action, and biochemical alterations produced by a novel molecule, 4-nitrobenzaldehyde thiosemicarbazone (BZTS), derived from S-limonene against Leishmania amazonensis. BZTS inhibited the growth of the promastigote and axenic amastigote forms, with an IC50 of 3.8 and 8.0 μM, respectively. Intracellular amastigotes were inhibited by the compound with an IC50 of 7.7 μM. BZTS also had a CC50 of 88.8 μM for the macrophage strain J774A1. BZTS altered the shape, size, and ultrastructure of the parasites, including damage to mitochondria, reflected by extensive

Iron chelators of the di-2-pyridylketone thiosemicarbazone and 2-benzoylpyridin e thiosemicarbazone series inhibit HIV-1 transcription: identification of novel cellular targets--iron, cyclin-dependent kinase (CDK) 2, and CDK9. Mol Pharmacol., Vol.79, No.1 (Jan 2011): 185-96. Debebe Z, Tatyana Ammosova, Breuer D, Lovejoy DB, Kalinowski DS, Karla PK, Kumar K, Jerebtsova M, Ray P, Kashanchi F, Victor R. Gordeuk, Richardson DR, Sergei Nekhai.. ...

Iron chelators of the di-2-pyridylketone thiosemicarbazone and 2-benzoylpyridin e thiosemicarbazone series inhibit HIV-1 transcription: identification of novel cellular targets--iron, cyclin-dependent kinase (CDK) 2, and CDK9. Mol Pharmacol., Vol.79, No.1 (Jan 2011): 185-96. Debebe Z, Tatyana Ammosova, Breuer D, Lovejoy DB, Kalinowski DS, Karla PK, Kumar K, Jerebtsova M, Ray P, Kashanchi F, Victor R. Gordeuk, Richardson DR, Sergei Nekhai.. ...

TY - CONF. T1 - Antitumor effects of novel co-drugs linking histone deacetylase and ribonucleotide reductase inhibitors in hematological tumors. AU - DAlessandro, Natale. AU - Ferro, Arianna. AU - Dusonchet, Luisa. AU - Meli, Maria. PY - 2011. Y1 - 2011. N2 - Combination therapy is the mainstay of anticancer therapy due to the significant synergistic effects achievable. Now that anticancer drug research turned toward a more molecular targeted approach, the design of dual-target drugs appears to be a new promising strategy with the potential to improve the therapeutic efficacy of the single drug and to reduce the probability of drug induced resistance and cross resistance. In our previous work, we found that 3-C-methyl-adenosine (3-Me-Ado), developed by us as a potent ribonucleotide reductase (RR) inhibitor with antitumor activity against both human leukemia and carcinoma cell lines, elicited significant growth inhibitory and apoptotic synergistic effects in promyelocytic leukemia cells in ...

This is the third volume of the Patent eBook Series entitled Topics in Anti-Cancer Research. This eBook comprises updated reviews on topics relevant to modern cancer research published in the journal Recent Patents on Anti-Cancer Drug Discovery. The comprehensive range of themes covered in this third volume will be of benefit to clinicians, scientists and R&D experts looking for new targets for the prevention of cancer and discovery of drugs for the treatment of different cancer types. Regulation of tumor cells by TRAIL receptors, development of anti- cancer drugs & immunomodulatory drugs, molecular studies of adrenocortical cancer, role of inhibitors of inosine monophosphate dehydrogenase in cancer, recent updates in glioblastoma stem cells, latest approaches for cancer gene therapy and metabolic therapy for cancer were reviewed and updated. The role of pH regulation and application of hyperthermia, thiosemicarbazone derivatives, tamoxifen-based therapies for cancer treatment andproteome-based ...

The electronic structure and the participation of the simplest azomethine imine (AI) in [3+2] cycloaddition (32CA) reactions have been analysed within the Molecular Electron Density Theory (MEDT) using Density Functional Theory (DFT) calculations at the MPWB1K/6-311G(d) level. Topological analysis of the electron localisation function reveals that AI has a pseudoradical structure, while the conceptual DFT reactivity indices characterises this three-atom-component (TAC) as a moderate electrophile and a good nucleophile. The non-polar 32CA reaction of AI with ethylene takes place through a one-step mechanism with moderate activation energy, 8.7 kcal·mol−1. A bonding evolution theory study indicates that this reaction takes place through a non-concerted [2n + 2τ] mechanism in which the C-C bond formation is clearly anticipated prior to the C-N one. On the other hand, the polar 32CA reaction of AI with dicyanoethylene takes place through a two-stage one-step mechanism. Now, the activation energy is only

N-(3-phenylpropyl)-1,2,3-benzotriazin-4-amine 1,3,2,4-Dithiaboretane, 2,4-difluoro- anthracen-9-ylmethyl N-octylcarbamate 2H-1-Benzopyran-5-carboxylic acid,3,4-dihydro-6,7-dihydroxy-3-[(1Z)-1- hydroxy-3-oxo-1-butenyl]-4-oxo- Ethanethiol, 2,2-(1,2-ethanediylbis(oxy))bis-, polymer with 1,1-(diisocyanatomethylene)bis(benzene), ethenyldiethoxymethylsilane, alpha-hydro-omega-hydroxypoly(oxy(methyl-1,2-ethanediyl)), alpha,alpha,alpha-1,2,3-propanetriyltris(omega-hydroxypoly(oxy(methyl-1,2-ethanediyl))) and 2-propen-1-ol [(amino-pyridin-2-yl-methylidene)amino] 3-iodobenzoate Dicyandiamide, hexamethylenetetramine, oleic acid reaction product 1,2,4-Methenocyclopenta[cd]pentalene-5-carboxaldehyde,2,2a,3,3,4,7-hexachlorodecahydro-,(1R,2R,2aR,4S,4aS,5R,6aR,6bR,7S)-rel- Dioctylbis(palmitoyloxy)stannane (2-(Hexahydro-3,5-dimethyl-1H-azepin-1-yl)ethyl)guanidine sulfate

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There is disclosed a process for the photochemical stabilization of dyed polyamide fibre materials, which comprises treating the dyed material with an aqueous foamed composition which contains at least a non-dyeing copper complex of bisazomethines, acylhydrazones, semicarbazones or thiosemicarbazones of aromatic aldehydes or ketones or oximes. By means of the process of this invention it is possible to prevent wastewater from being contaminated with copper-containing impurities.

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The first catalytic asymmetric [3+3] cycloaddition of azomethine ylides with C3-substituted 2-indolylmethanols has been established, leading to diastereo- and enantioselective construction of a tetrahydropyrimido[1,6-a]indole framework (up to 91% yield, %3E95:5 dr, 98:2 er). This reaction also represents a new type of catalytic enantioselective [3+3] cycloaddition using azomethine ylides.

The metal chelating compound Dp44mT is a di-2-pyridylketone thiosemicarbazone (DpT) which displays potent and selective anti-tumor activity. This compound is receiving translational attention but its mechanism is poorly understood. Here we report that Dp44mT targets lysosome integrity through copper binding. Studies using the lysosomotropic fluorochrome acridine orange established that the copper-Dp44mT complex (Cu[Dp44mT]) disrupted lysosomes. This targeting was confirmed with pepstatin A-BODIPY FL, which showed re-distribution of cathepsin D to the cytosol with ensuing cleavage of the pro-apoptotic BH3 protein Bid. Redox activity of Cu[Dp44mT] caused cellular depletion of glutathione and lysosomal damage was prevented by co-treatment with the glutathione precursor N-acetylcysteine. Copper binding was essential for the potent anti-tumor activity of Dp44mT, since co-incubation with non-toxic copper chelators markedly attenuated its cytotoxicity. Taken together, our studies show how the lysosomal ...

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Flotation-separation of toxic metal ions from aqueous solutions using thiosemicarbazide derivatives as chelating agents and oleic acid as a surfactant

Two novel square planar complexes [Ni(Hapt)2] (1) and [Ni(btsc)] (2) have been synthesized from acetone N4-phenyl-thiosemicarbazone (Hapt) and benzoyl-3-thiosemicarbazide (Hbtsc) by the reaction of nickel(ii) salt. The ligand and complexes have been characterized by various physicochemical methods. Complexes

Four new neutral copper azido polymers, Cu-4(N-3)(8)(L-1)(2)](n) (1), Cu-4(N-3)(8)(L-2)(2)](n) (2), Cu-4(N-3)(8)(L-3)(2)](n) (3), and Cu-9(N-3)(18)(L-4)(4)](n) (4) L1-4 are formed in situ by reacting pyridine-2-carboxaldehyde with 22-(methylamino)ethyl]pyridine (mapy, L-1), N,N-dimethylethylenediamine (N,N-dmen, L-2), N,N-diethylethylenediamine (N,N-deen, L-3), and N,N,2,2-tetramethylpropanediamine (N,N,2,2-tmpn, L-4)], have been synthesized by using 0.5 mol equiv of the chelating tridentate ligands with Cu-(NO3)(2)center dot 3H(2)O and an excess of NaN3. Single-crystal X-ray structures show that the basic unit of these complexes, especially 1-3, contains very similar Cu-4(II) building blocks. The overall structure of 3 is two-dimensional, while the other three complexes are one-dimensional in nature. Complex 1 represents a unique example containing hemiaminal ether arrested by copper(R). Complexes 1 and 2 have a rare bridging azido pathway: both end-on and end-to-end bridging azides between a ...

Authors: ASGHAR DAVOOD, ESKANDAR ALIPOUR, ABBAS SHAFIEE Abstract: 4(5)-Chloro-imidazole-5(4)-carboxaldehyde derivatives are important precursors for the preparation of biologically active compounds. We developed a simple, novel, and efficient method for the synthesis of these compounds. The chemistry described is amenable to large-scale use and is flexible enough to allow the preparation of analogs. Keywords: Imidazole, N-chlorosuccinimide, chloroimidazole, chloroimidazole-carboxaldehyde Full Text: PDF ...

-Cymene; 2,5-Dimethylpyrrole; Acetoin, ≥96%, FCC, FG; 2,5-Dimethylpyrazine; 2,6-Dimethylpyrazine; 2-Ethylpyrazine, ≥98%, FG; 2,3-Dimethylpyrazine; 4-Heptanone; 3-Ethylpyridine; 2,3,5-Trimethylpyrazine; Furfural; Pyrrole; Furfuryl acetate; Linalool; Linalyl acetate; 5-Methylfurfural; γ-Butyrolactone; 2-Acetyl-1-methylpyrrole; Furfuryl alcohol; 2-Acetylpyrrole; Pyrrole-2-carboxaldehyde