• 제목/요약/키워드: Ligand Effects

검색결과 404건 처리시간 0.024초

Synthesis of N,N-Diaryl-(pyridin-3-yl)pyrimidin-2-amine Derivatives and Their Photochemical Properties

  • El-Deeb, Ibrahim Mustafa;Lee, So-Ha
    • 한국응용과학기술학회지
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    • 제25권3호
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    • pp.291-298
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    • 2008
  • Although the pyrimidine derivatives were obtained in low yields ranging from 8% to 20%, we reported the successful preparation of N,N-diaryl-pyrimidin-2-amine derivatives starting from the corresponding 2-aminopyrimidines (1a-1c), by direct palladium-catalyzed arylation using different arylbromides. The reasons of low yields are thought to be the electronic and steric effects by the neighboring aromatic systems. The absorption spectra and photoluminescent spectra of compounds (3a 3g and 4a-4c) were measured using dichloromethane on the concentration of 25 mM by UV vis spectroscopy and luminescent spectroscopy. Pyrimidine derivatives 4a, 4b, and 4c showed moderate emission maxima at 474 nm, 481 nm, and 367 nm, respectively, while other compounds showed very weak photoluminescence or no photoluminescence at all.

Diaminocyclohexane을 배위자로 한 새로운 항암성 백금(II)착체류의 일반약리작용 (General Pharmacology of the New Platinum (II) Anticancer Agents with Diaminocyclohexane as a Carrier Ligand)

  • 고석태;강선영;임동윤;신현준;최승기;노영수;정지창
    • Biomolecules & Therapeutics
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    • 제6권3호
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    • pp.303-311
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    • 1998
  • The general pharmacological properties of new platinum (II) coordination complexes, SA : [Pt(trans-ι-DACH)(DPPE)] . 2NO$_3$, SB : [Pt(cia-DACH)(DPPP)] 2NO$_3$ and SC : [Pt(cia-DACH)(DPPE)] 2NO$_3$on central nervous, respiratory, cardiovascular and digestive systems were studied in various experimental animals. These platinum (II) anticancer agents had no effects on analgesia, thiopental-induced sleeping time, body temperature, strychnine-induced convulsion, inflammation and local anesthetic action in mice and rats. Intestinal motility, stomach-ulcer induced by serotonin and bile-secretion of rats were not influenced by the dose of 30 mg/kg. However SB and SC induced a mild decrease in heart rate in anesthetized rats. Based on these results, these new platinum (II) complexes may be regarded as a valuable lead compound in the development of new anticancer chemotherapeutic agents with marked antitumor activity and low toxicity.

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Reactivity of Functional Food Substance in terms of Structure Analysis

  • Kwon, Dae-Young
    • 한국식품위생안전성학회:학술대회논문집
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    • 한국식품위생안전성학회 2003년도 추계 국제심포지움 및 학술발표회
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    • pp.46-46
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    • 2003
  • Hypocholesterolemic peptide isolated from glycimin (11S protein) hydrolyzate by trypsin was purified and identified as LPYP and IAVPGEVA. To investigate the effects of phyiscal properties of side chains of the hypocholesterolemic activity, some of mutant peptides were designed and synthesized chemically. The structure related structures of each peptide were simulated and constructed and their conformations were observed by using spectropolarimeter. The hypocholesterolemic activities were monitored by assaying the inhibition of 3-hydroxy-3-methylglutaryl CoA reductase (HMG-CoA reductase) in vitro and by the determination of cholesterol content in mice serum. For LPYP derivatives, Hypocholesterolemic activity was lost when hydrophobic leucine residue at N-terminus was not so critical for maintaining hypocholesterolemic activity. For idealogical design of hypocholesterolemic peptides, the structure of HMG-CoA reductase are shown and inhibition mechanism of some peptides or inhibitors will be presented. For IAVPGEVA derivative inhibition of HMG-CoA reductase has been studied. For detail study of hypocholesterolemic activity, kinetic study of inhibition of peptides on HMG-CoA reductase and structural view of ligand binding should be investigated.

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생체모방계에 의한 시클로헥산 산화반응에서 리간드의 영향 (Influence of Ligand on Oxidation of Cyclohexane in the Biomimetic System)

  • 김성보
    • Korean Chemical Engineering Research
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    • 제43권2호
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    • pp.202-205
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    • 2005
  • GoAgg 생체모방계 산화반응시스템을 이용하여 상온, 상압에서 시크로헥산을 산화 반응하여 시크로헥산올과 시클로헥산온 제조를 위한 연구를 수행하였다. 반응속도론적 연구를 수행하였으며 리간드로 카르복실기를 포함하는 picolinic acid를 사용한 경우 철 촉매만 사용한 경우에 비해 15배 이상의 활성이 증가하였다. 특히 피리딘환이나 이미다졸환에 ortho 위치에 카르복실기를 포함한 경우 meta, para 위치보다 반응성이 크게 증가하였다. 이 결과로부터 새로운 매커니즘을 제안하였다.

Sorbent Extraction of Some Metal Ions on a Gas Chromatographic Stationary Phase Prior to Their Flame Atomic Absorption Determinations

  • Soylak, M.;Saracoglu, S.;Elci, L.
    • Bulletin of the Korean Chemical Society
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    • 제24권5호
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    • pp.555-558
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    • 2003
  • An enrichment/separation system for atomic absorption spectrometric determinations of Cu(Ⅱ), Fe(Ⅲ), Ni(Ⅱ) and Co(Ⅱ) has been established. The procedure is based on the adsorption of the analytes as calmagite chelates on Chromosorb-102. The effects of some parameters including pH, amount of ligand, salt matrix, flow rates of sample and eluent solutions were investigated. Under optimized conditions, the relative standard deviation of the combined method of sample treatment, preconcentration and determination with FAAS (N=5) is generally lower than 5%. The limit of detection (3σ) was between 6.0-112.9 ㎍/L. The results were used for preconcentration of analytes from some sodium and ammonium salt.

Adsorption of Rare Earth Metal Ion on N-Phenylaza-15-Crown-5 Synthetic Resin with Styrene Hazardous Material

  • Kim, Se-Bong;Kim, Joon-Tae
    • 통합자연과학논문집
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    • 제7권2호
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    • pp.130-137
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    • 2014
  • Resins were synthesized by mixing N-phenylaza-15-crown-5 macrocyclic ligand attached to styrene (2th petroleum in 4th class hazardous materials) divinylbenzene (DVB) copolymer with crosslink of 1%, 2%, 6%, and 12% by substitution reaction. The synthesis of these resins was confirmed by content of chlorine, element analysis, thermo gravimetric analysis (TGA), surface area, and IR-spectroscopy. The effects of pH, equilibrium arrival time, dielectric constant of solvent and crosslink on adsorption of metal ions by the synthetic resin adsorbent were investigated. The metal ions were showed fast adsorption on the resins above pH 4. The optimum equilibrium time for adsorption of metallic ions was about two hours. The adsorption selectivity determined in ethanol was in increasing order uranium (VI) > zinc (II) > europium (III) ions. The uranium ion adsorbed in the order of 1%, 2%, 6%, and 12% crosslink resin and adsorption of resin decreased in proportion to the order of dielectric constant of solvents.

Receptor for Advanced Glycation Endproducts (RAGE), Its Ligands, and Soluble RAGE: Potential Biomarkers for Diagnosis and Therapeutic Targets for Human Renal Diseases

  • Lee, Eun Ji;Park, Jong Hoon
    • Genomics & Informatics
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    • 제11권4호
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    • pp.224-229
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    • 2013
  • Receptor for advanced glycation endproducts (RAGE) is a multi-ligand receptor that is able to bind several different ligands, including advanced glycation endproducts, high-mobility group protein (B)1 (HMGB1), S-100 calcium-binding protein, amyloid-${\beta}$-protein, Mac-1, and phosphatidylserine. Its interaction is engaged in critical cellular processes, such as inflammation, proliferation, apoptosis, autophagy, and migration, and dysregulation of RAGE and its ligands leads to the development of numerous human diseases. In this review, we summarize the signaling pathways regulated by RAGE and its ligands identified up to date and demonstrate the effects of hyper-activation of RAGE signals on human diseases, focused mainly on renal disorders. Finally, we propose that RAGE and its ligands are the potential targets for the diagnosis, monitoring, and treatment of numerous renal diseases.

꾸지뽕나무 뿌리 추출물의 파골세포 분화 억제 효과 (Inhibitory Effects of the Roots of Cudrania tricuspidata Bureau on Osteoclast Differentiation)

  • 김유경;정길생
    • 생약학회지
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    • 제48권2호
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    • pp.155-159
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    • 2017
  • Cudrania tricuspidata Bureau (Moraceae) is a traditional oriental medicine that has been widely used as anti-oxidant, anti-inflammatory and immunomodulatory in Korea. This study was performed that the 70% ethanol extract of the roots of C. tricuspidata (CTE) suppressed receptor activator of NF-${\kappa}B$ ligand (RANKL)-induced osteoclastogenesis, actin ring formation in RAW 264.7 cell lines. CTE significantly inhibited the JNK/mitogen-activated protein kinase (MAPK) signaling pathway without affecting ERK and p38 signaling in RANKL-stimulated RAW 264.7 cells. Also, CTE inhibited RANKL-induced expression of c-Fos, an upstream activator of NFATc1. Consequently, CTE suppresses osteoclast differentiation by inhibiting RANKL induced MAPK signaling pathways and disrupts the actin rings in mature osteoclasts. Thus, CTE can be used for the development of osteoporosis treatment drug with a natural material.

Regulation of Cyp 1A1 Gene Expression by Retinoic Acid Receptor, Retinoid X Receptor and Constitutive Androstane Receptor in Rainbow Trout Hepatoma Cells(Rth 149)

  • Kim, Ji-Sun;Yang, So-Yeun;Seo, Mi-Jung;Sheen, Yhun-Yhong
    • 한국독성학회:학술대회논문집
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    • 한국독성학회 2003년도 추계학술대회
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    • pp.136-136
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    • 2003
  • Exposure of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) causes a variety of biological and toxicology effects, most of which are mediated by aryl hydrocarbon receptor (AhR). The ligand-bound AhR as a heterodimer with AhR nuclear translocator (ARNT) binds to its specific DNA recognition site, the dioxin-responsive element (DRE), and it results in increased transcription of CVP1A1 gene.(omitted)

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Template Synthesis of New Nickel(Ⅱ) Comlexes of 14-Membered Pentaaza Macrocyclic Ligands: Effects of C-Alkyl and N-Hydroxyalkyl Pendant Arms on the Solution Behaviors of the Complexes

  • 강신걸;최장식;김성진
    • Bulletin of the Korean Chemical Society
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    • 제16권6호
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    • pp.518-523
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    • 1995
  • New square planar nickel(Ⅱ) complexes with various 1-alkyl (4a-4c) and 1-hydroxyalkyl (4d-4f) derivatives of the 14-membered pentaaza macrocycle 8-ethyl-8-nitro-1,3,6,10,13-pentaazacyclotetradecane have been synthesized by two-step metal template condensation reactions of ethylenediamine, nitroethane, formaldehyde, and appropriate primary amines. The nitro group and/or hydroxyl group of 4a-4f are not directly involved in the coordination. The nickel(Ⅱ) complexes exist in coordinating solvents such as MeCN, Me2SO, and H2O as equilibrium mixtures of the square planar [Ni(L)]2+(L=4a-4f) and octahedral species [Ni(L)S2]2+(S=solvent molecule). Although the ligand field strength and redox potentials of the complexes are not affected by the nature of the substituents, the formation of octahedral species for 4d-4f in MeCN is strongly restricted by the hydroxyl group. Synthesis, characterization, and solution behaviors of the nickel(Ⅱ) complexes are described.