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  1 / 9311 MEDLINE  
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[PMID]:29455554
[Au] Autor:El-Husseiny WM; El-Sayed MA; Abdel-Aziz NI; El-Azab AS; Ahmed ER; Abdel-Aziz AA
[Ad] Endereço:a Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy , Mansoura University , Mansoura , Egypt.
[Ti] Título:Synthesis, antitumour and antioxidant activities of novel α,ß-unsaturated ketones and related heterocyclic analogues: EGFR inhibition and molecular modelling study.
[So] Source:J Enzyme Inhib Med Chem;33(1):507-518, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:New α,ß-unsaturated ketones 4a,b; 5a-c; and 6a,b; as well as 4-H pyran 7; pyrazoline 8a,b; isoxazoline 9; pyridine 10-11; and quinoline-4-carboxylic acid 12a,b derivatives were synthesized and evaluated for in vitro antitumour activity against HepG2, MCF-7, HeLa, and PC-3 cancer cell lines. Antioxidant activity was investigated by the ability of these compounds to scavenge the 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation (ABTS ). Compounds 6a, 6b, 7, and 8b exhibited potent antitumour activities against all tested cell lines with [IC ] ≅5.5-18.1 µΜ), in addition to significantly high ABTS scavenging activities. In vitro EGFR kinase assay for 6a, 6b, 7, and 8b as the most potent antitumour compounds showed that; compounds 6b, and 7 exhibited worthy EGFR inhibition activity with IC values of 0.56 and 1.6 µM, respectively, while compounds 6a and 8b showed good inhibition activity with IC values of 4.66 and 2.16 µM, respectively, compared with sorafenib reference drug (IC = 1.28 µM). Molecular modelling studies for compounds 6b, 7, and 8b were conducted to exhibit the binding mode towards EGFR kinase, which showed similar interaction with erlotinib.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Antioxidantes/farmacologia
Compostos Heterocíclicos/farmacologia
Cetonas/farmacologia
Inibidores de Proteínas Quinases/farmacologia
Receptor do Fator de Crescimento Epidérmico/antagonistas & inibidores
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Antioxidantes/síntese química
Antioxidantes/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Compostos Heterocíclicos/síntese química
Compostos Heterocíclicos/química
Seres Humanos
Cetonas/síntese química
Cetonas/química
Modelos Moleculares
Estrutura Molecular
Inibidores de Proteínas Quinases/síntese química
Inibidores de Proteínas Quinases/química
Receptor do Fator de Crescimento Epidérmico/metabolismo
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Antioxidants); 0 (Heterocyclic Compounds); 0 (Ketones); 0 (Protein Kinase Inhibitors); EC 2.7.10.1 (Receptor, Epidermal Growth Factor)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180227
[Lr] Data última revisão:
180227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180220
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2018.1434519


  2 / 9311 MEDLINE  
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[PMID]:29311461
[Au] Autor:Nambu H
[Ad] Endereço:Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama.
[Ti] Título:[Novel Methods for the Synthesis of Heterocycles Using Highly Reactive Spirocyclopropanes].
[So] Source:Yakugaku Zasshi;138(1):19-25, 2018.
[Is] ISSN:1347-5231
[Cp] País de publicação:Japan
[La] Idioma:jpn
[Ab] Resumo:This review describes our recent efforts to develop efficient methods for the synthesis of heterocyclic compounds, such as indoles and benzofurans, employing ring-opening cyclization of cyclohexane-1,3-dione-2-spirocyclopropanes, which were prepared by the reaction of 1,3-cyclohexanediones with sulfonium salts. Ring-opening cyclization of cyclohexane-1,3-dione-2-spirocyclopropanes with primary amines proceeded at room temperature to provide 2-substituted tetrahydroindol-4(5H)-ones in good to excellent yield. The obtained product was readily converted into a 2-substituted 4-hydroxyindole derivative. Furthermore, acid-catalyzed ring-opening cyclization of cyclohexane-1,3-dione-2-spirocyclopropanes proceeded smoothly at room temperature to provide 2-substituted tetrahydrobenzofuran-4(2H)-ones in excellent yield. The obtained product was converted into a 2-substituted 4-hydroxybenzofuran derivative. The synthetic utility of this catalytic protocol was demonstrated by the total synthesis of cuspidan B.
[Mh] Termos MeSH primário: Química Orgânica/métodos
Compostos Heterocíclicos/síntese química
[Mh] Termos MeSH secundário: Aminas/química
Benzofuranos/síntese química
Catálise
Ciclização
Cicloexanos/síntese química
Cicloexanonas/química
Ciclopropanos/síntese química
Indóis/síntese química
Fenômenos de Química Orgânica
Alimentos de Soja
Estilbenos/síntese química
Compostos de Sulfônio/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Amines); 0 (Benzofurans); 0 (Cyclohexanes); 0 (Cyclohexanones); 0 (Cyclopropanes); 0 (Heterocyclic Compounds); 0 (Indoles); 0 (Stilbenes); 0 (Sulfonium Compounds); 0 (cuspidan B); 6UK3D2BXJT (1,3-cyclohexanedione)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180110
[St] Status:MEDLINE
[do] DOI:10.1248/yakushi.17-00188


  3 / 9311 MEDLINE  
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[PMID]:29249626
[Au] Autor:Sekioka R; Honjo E; Honda S; Fuji H; Akashiba H; Mitani Y; Yamasaki S
[Ad] Endereço:Drug Discovery Research, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan. Electronic address: ryuichi.sekioka@astellas.com.
[Ti] Título:Discovery of novel scaffolds for γ-secretase modulators without an arylimidazole moiety.
[So] Source:Bioorg Med Chem;26(2):435-442, 2018 01 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Gamma-secretase modulators (GSMs) selectively inhibit the production of amyloid-ß 42 (Aß42) and may therefore be useful in the management of Alzheimer's disease. Most heterocyclic GSMs that are not derived from nonsteroidal anti-inflammatory drugs contain an arylimidazole moiety that potentially inhibits cytochrome P450 (CYP) activity. Here, we discovered imidazopyridine derivatives that represent a new class of scaffold for GSMs, which do not have a strongly basic end group such as arylimidazole. High-throughput screening identified 2-methyl-8-[(2-methylbenzyl)oxy]-3-(pyridin-4-yl)imidazo[1,2-a]pyridine (3a), which inhibited the cellular production of Aß42 (IC = 7.1 µM) without changing total production of Aß. Structural optimization of this series of compounds identified 5-[8-(benzyloxy)-2-methylimidazo[1,2-a]pyridin-3-yl]-2-ethylisoindolin-1-one (3m) as a potent inhibitor of Aß42 (IC = 0.39 µM) but not CYP3A4. Further, 3m demonstrated a sustained pharmacokinetic profile in mice and sufficiently penetrated the brain.
[Mh] Termos MeSH primário: Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores
Descoberta de Drogas
Compostos Heterocíclicos/farmacologia
Imidazóis/farmacologia
Piridinas/farmacologia
[Mh] Termos MeSH secundário: Administração Oral
Secretases da Proteína Precursora do Amiloide/metabolismo
Peptídeos beta-Amiloides/antagonistas & inibidores
Peptídeos beta-Amiloides/biossíntese
Animais
Linhagem Celular Tumoral
Citocromo P-450 CYP3A/metabolismo
Relação Dose-Resposta a Droga
Compostos Heterocíclicos/administração & dosagem
Compostos Heterocíclicos/química
Seres Humanos
Imidazóis/administração & dosagem
Imidazóis/química
Injeções Intraperitoneais
Masculino
Camundongos
Camundongos Endogâmicos
Microssomos Hepáticos/química
Microssomos Hepáticos/metabolismo
Modelos Moleculares
Estrutura Molecular
Fragmentos de Peptídeos/antagonistas & inibidores
Fragmentos de Peptídeos/biossíntese
Piridinas/administração & dosagem
Piridinas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amyloid beta-Peptides); 0 (Heterocyclic Compounds); 0 (Imidazoles); 0 (Peptide Fragments); 0 (Pyridines); 0 (amyloid beta-protein (1-42)); 0 (imidazopyridine); EC 1.14.14.1 (Cytochrome P-450 CYP3A); EC 1.14.14.1 (cytochrome P450 3A4, mouse); EC 3.4.- (Amyloid Precursor Protein Secretases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180220
[Lr] Data última revisão:
180220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171219
[St] Status:MEDLINE


  4 / 9311 MEDLINE  
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[PMID]:28463762
[Au] Autor:Paixão DA; Marzano IM; Jaimes EHL; Pivatto M; Campos DL; Pavan FR; Deflon VM; Maia PIDS; Da Costa Ferreira AM; Uehara IA; Silva MJB; Botelho FV; Pereira-Maia EC; Guilardi S; Guerra W
[Ad] Endereço:Instituto de Química, Universidade Federal de Uberlândia, Uberlândia, MG, Brazil.
[Ti] Título:Novel copper(II) complexes with hydrazides and heterocyclic bases: Synthesis, structure and biological studies.
[So] Source:J Inorg Biochem;172:138-146, 2017 Jul.
[Is] ISSN:1873-3344
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Five new copper(II) complexes of the type [Cu(NO)(NN)(ClO ) ], in which NO=4-fluorophenoxyacetic acid hydrazide (4-FH) or 4-nitrobenzoic hydrazide (4-NH) and NN=1,10-phenanthroline (phen), 4-4'-dimethoxy-2-2'-bipyridine (dmb) or 2,2-bipyridine (bipy) were synthesized and characterized using various spectroscopic methods. The X-ray structural analysis of one representative compound indicates that the geometry around the copper ion is distorted octahedron, in which the ion is coordinated to hydrazide via the terminal nitrogen and the carbonyl oxygen, and to heterocyclic bases via their two nitrogen atoms. Two perchlorate anions occupy the apical positions, completing the coordination sphere. The cytotoxic activity of compounds was investigated in three tumor cell lines (K562, MDA-MB-231 and MCF-7). Concerning K562 cell line, the complexes with 1,10-phenanthroline exhibit high cytotoxic activity and are more active than carboplatin, free ligands and [Cu(phen) ] . Considering the cytotoxicity results, further investigations for the compounds [Cu(4-FH)(phen)(ClO ) ] I and [Cu(4-NH)(phen)(ClO ) ]∙H O III were performed. Flow cytometric analysis revealed that these complexes induce apoptotic cell death in MDA-MB-231 cell line and bind to DNA with K values of 4.38×10 and 2.62×10 , respectively. These compounds were also evaluated against wild type Mycobacterium tuberculosis (ATCC 27294) and exhibited antimycobacterial activity, displayed MIC values lower than those of the corresponding free ligands.
[Mh] Termos MeSH primário: Complexos de Coordenação/síntese química
Complexos de Coordenação/farmacologia
Cobre/química
Compostos Heterocíclicos/química
Hidrazinas/química
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/farmacologia
Antituberculosos/síntese química
Antituberculosos/farmacologia
Apoptose/efeitos dos fármacos
Neoplasias da Mama/tratamento farmacológico
Linhagem Celular Tumoral
Complexos de Coordenação/química
Cristalografia por Raios X
Feminino
Seres Humanos
Concentração Inibidora 50
Células K562
Testes de Sensibilidade Microbiana
Estrutura Molecular
Mycobacterium/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Antitubercular Agents); 0 (Coordination Complexes); 0 (Heterocyclic Compounds); 0 (Hydrazines); 27RFH0GB4R (hydrazine); 789U1901C5 (Copper)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180220
[Lr] Data última revisão:
180220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE


  5 / 9311 MEDLINE  
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[PMID]:29248295
[Au] Autor:Zhang E; Wang MM; Huang SC; Xu SM; Cui DY; Bo YL; Bai PY; Hua YG; Xiao CL; Qin S
[Ad] Endereço:School of Pharmaceutical Sciences, Institute of Drug Discovery and Development, Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Zhengzhou University, Zhengzhou 450001, PR China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Pr
[Ti] Título:NOTA analogue: A first dithiocarbamate inhibitor of metallo-ß-lactamases.
[So] Source:Bioorg Med Chem Lett;28(2):214-221, 2018 01 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The emergence of antibiotic drug (like carbapenem) resistance is being a global crisis. Among those resistance factors of the ß-lactam antibiotics, the metallo-ß-lactamases (MBLs) is one of the most important reasons. In this paper, a series of cyclic dithiocarbamate compounds were synthesized and their inhibition activities against MBLs were initially tested combined with meropenem (MEM) by in vitro antibacterial efficacy tests. Sodium 1,4,7-triazonane-1,4,7-tris(carboxylodithioate) (compound 5) was identified as the most active molecule to restore the activity of MEM. Further anti-bacterial effectiveness assessment, compound 5 restored the activity of MEM against Escherichia coli, Citrobacter freundii, Proteus mirabilis and Klebsiella pneumonia, which carried resistance genes of bla . The compound 5 was non-hemolytic, even at a concentration of 1000 µg/mL. This compound was low toxic toward mammalian cells, which was confirmed by fluorescence microscopy image and the inhibition rate of HeLa cells. The Ki value of compounds 5 against NDM-1 MBL was 5.63 ±â€¯1.27 µM. Zinc ion sensitivity experiments showed that the inhibitory effect of compound 5 as a MBLs inhibitor was influenced by zinc ion. The results of the bactericidal kinetics displayed that compound 5 as an adjuvant assisted MEM to kill all bacteria. These data validated that this NOTA dithiocarbamate analogue is a good inhibitor of MBLs.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Compostos Heterocíclicos/farmacologia
Inibidores de beta-Lactamases/farmacologia
beta-Lactamases/metabolismo
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Sobrevivência Celular/efeitos dos fármacos
Citrobacter freundii/efeitos dos fármacos
Relação Dose-Resposta a Droga
Escherichia coli/efeitos dos fármacos
Células HeLa
Compostos Heterocíclicos/síntese química
Compostos Heterocíclicos/química
Seres Humanos
Klebsiella pneumoniae/efeitos dos fármacos
Testes de Sensibilidade Microbiana
Estrutura Molecular
Proteus mirabilis/efeitos dos fármacos
Relação Estrutura-Atividade
Inibidores de beta-Lactamases/síntese química
Inibidores de beta-Lactamases/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Heterocyclic Compounds); 0 (beta-Lactamase Inhibitors); 56491-86-2 (1,4,7-triazacyclononane-N,N',N''-triacetic acid); EC 3.5.2.6 (beta-Lactamases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171218
[St] Status:MEDLINE


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[PMID]:29233652
[Au] Autor:Wang S; Gai Y; Zhang S; Ke L; Ma X; Xiang G
[Ad] Endereço:School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, Hubei, China.
[Ti] Título:Synthesis and evaluation of a class of 1,4,7-triazacyclononane derivatives as iron depletion antitumor agents.
[So] Source:Bioorg Med Chem Lett;28(2):117-121, 2018 01 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Iron depletion has been confirmed as an efficient strategy for cancer treatment. In the current study, a series of 1,4,7-triazacyclononane derivatives HE-NO2A, HP-NO2A and NE2P2A, as well as the bifunctional chelators p-NO -PhPr-NE3TA and p-NH -PhPr-NE3TA were synthesized and evaluated as iron-depleting agents for the potential anti-cancer therapy against human hepatocellular carcinoma. The cytotoxicity of these chelators was measured using hepatocellular cancer cells and compared with the clinically available iron depletion agent DFO and the universal metal chelator DTPA. All these 1,4,7-triazacyclononane-based chelators exhibited much stronger antiproliferative activity than DFO and DTPA. Among them, chelators with phenylpropyl side chains, represented by p-NO -PhPr-NE3TA and p-NH -PhPr-NE3TA, displayed the highest antiproliferative activity against HepG2 cells. Hence, these compounds are attractive candidates for the advanced study as iron depletion agents for the potential anti-cancer therapy, and could be further in conjugation with a targeting moiety for the future development in targeted iron depletion therapy.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Quelantes/farmacologia
Compostos Heterocíclicos/farmacologia
Ferro/metabolismo
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Proliferação Celular/efeitos dos fármacos
Quelantes/síntese química
Quelantes/química
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Células Hep G2
Compostos Heterocíclicos/síntese química
Compostos Heterocíclicos/química
Seres Humanos
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Chelating Agents); 0 (Heterocyclic Compounds); 4730-54-5 (1,4,7-triazacyclononane); E1UOL152H7 (Iron)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171214
[St] Status:MEDLINE


  7 / 9311 MEDLINE  
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[PMID]:29235831
[Au] Autor:Osadchuk TV; Shybyryn OV; Kibirev VK
[Ti] Título:Chemical structure and properties of low-molecular furin inhibitors.
[So] Source:Ukr Biochem J;88(6):5-25, 2016 Nov-Dec.
[Is] ISSN:2409-4943
[Cp] País de publicação:Ukraine
[La] Idioma:eng
[Ab] Resumo:The review is devoted to the analysis of the relationship between a chemical structure and properties of low-molecular weight inhibitors of furin, the most studied proprotein convertase, which is involved in the development of some pathologies, such as oncologic diseases, viral and bacterial infections, etc. The latest data concerning the influence of peptides, pseudo-peptides, aromatic and heterocyclic compounds, some natural ones such as flavonoids, coumarins, and others on enzyme inactivation are considered. The power of furin inhibition is shown to rise with the increasing number of positively charged groups in the structure of these compounds. Peptidomimetics (Ki = 5-8 pM) are shown to be the most effective furin inhibitors. The synthesized substances, however, have not been used in practical application yet. Nowadays it is very important to find more selective inhibitors, improve their stability, bioavailability and safety for the human organism.
[Mh] Termos MeSH primário: Cumarínicos/química
Flavonoides/química
Furina/antagonistas & inibidores
Compostos Heterocíclicos/química
Peptídeos/química
Peptidomiméticos/química
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Antibacterianos/farmacologia
Antineoplásicos/síntese química
Antineoplásicos/química
Antineoplásicos/farmacologia
Antivirais/síntese química
Antivirais/química
Antivirais/farmacologia
Cumarínicos/síntese química
Cumarínicos/farmacologia
Flavonoides/síntese química
Flavonoides/farmacologia
Furina/química
Furina/metabolismo
Compostos Heterocíclicos/síntese química
Compostos Heterocíclicos/farmacologia
Seres Humanos
Cinética
Peptídeos/síntese química
Peptídeos/farmacologia
Peptidomiméticos/síntese química
Peptidomiméticos/farmacologia
Inibidores de Proteases/síntese química
Inibidores de Proteases/química
Inibidores de Proteases/farmacologia
Eletricidade Estática
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antineoplastic Agents); 0 (Antiviral Agents); 0 (Coumarins); 0 (Flavonoids); 0 (Heterocyclic Compounds); 0 (Peptides); 0 (Peptidomimetics); 0 (Protease Inhibitors); EC 3.4.21.75 (Furin)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180116
[Lr] Data última revisão:
180116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171214
[St] Status:MEDLINE
[do] DOI:10.15407/ubj88.06.005


  8 / 9311 MEDLINE  
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[PMID]:27775528
[Au] Autor:Hou J; Luo T; Ng KL; Leung AY; Liang R; Sun D
[Ti] Título:Characterization of Drug Effect on Leukemia Cells Through Single Cell Assay With Optical Tweezers and Dielectrophoresis.
[So] Source:IEEE Trans Nanobioscience;15(8):820-827, 2016 12.
[Is] ISSN:1558-2639
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:One of the greatest challenges in acute myeloid leukemia (AML) treatment is preventing relapse. Leukemia cells can hide in bone marrow niche or vascular niche. Hence, many chemical drugs cannot kill these cells. To characterize migration and adhesion properties of leukemia cells in specific niches, CXCR4/SDF- 1α signal pathway has been widely used for investigation. AMD3100 is treated as one of the most common chemical drugs that can inhibit this signal. In the current study, we particularly investigate the effect of AMD3100 on the adhesion property of leukemia cells on stromal cells by using engineering tools, namely, optical tweezers (OT) and dielectrophoresis (DEP), to probe single cell property. AMD3100 not only inhibits the CXCR4/SDF- 1α signal pathway but also reduces gene expression of CXCR4 and VLA-4 on leukemia cells. The drug also softens leukemia cells. This work provides a new way to investigate cell behavior under drug treatment. The use of combined engineering tools will benefit drug discovery and assessment for leukemia treatment.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Eletroforese/métodos
Compostos Heterocíclicos/farmacologia
Leucemia Mieloide Aguda/metabolismo
Pinças Ópticas
Análise de Célula Única/métodos
[Mh] Termos MeSH secundário: Adesão Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Quimiocina CXCL12/análise
Quimiocina CXCL12/genética
Quimiocina CXCL12/metabolismo
Técnicas de Cocultura
Seres Humanos
Receptores CXCR4/análise
Receptores CXCR4/genética
Receptores CXCR4/metabolismo
Transdução de Sinais/efeitos dos fármacos
Células Estromais/citologia
Células Estromais/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (CXCR4 protein, human); 0 (Chemokine CXCL12); 0 (Heterocyclic Compounds); 0 (Receptors, CXCR4); 155148-31-5 (JM 3100)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171222
[Lr] Data última revisão:
171222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161025
[St] Status:MEDLINE
[do] DOI:10.1109/TNB.2016.2616160


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[PMID]:28464340
[Au] Autor:Aktas A; Taslimi P; Gülçin I; Gök Y
[Ad] Endereço:Faculty of Arts and Sciences, Department of Chemistry, Inönü University, Malatya, Turkey.
[Ti] Título:Novel NHC Precursors: Synthesis, Characterization, and Carbonic Anhydrase and Acetylcholinesterase Inhibitory Properties.
[So] Source:Arch Pharm (Weinheim);350(6), 2017 Jun.
[Is] ISSN:1521-4184
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Three series of imidazolidinium ligands (NHC precursors) substituted with 4-vinylbenzyl, 2-methyl-1,4-benzodioxane, and N-propylphthalimide were synthesized. N-Heterocyclic carbene (NHC) precursors were prepared from N-alkylimidazoline and alkyl halides. The novel NHC precursors were characterized by H NMR, C NMR, FTIR spectroscopy, and elemental analysis techniques. The enzymes inhibition activities of the NHC precursors were investigated against the cytosolic human carbonic anhydrase I and II isoenzymes (hCA I and II) and the acetylcholinesterase (AChE) enzyme. The inhibition parameters (IC and K values) were calculated by spectrophotometric method. The inhibition constants (K ) were found to be in the range of 166.65-635.38 nM for hCA I, 78.79-246.17 nM for hCA II, and 23.42-62.04 nM for AChE. Also, the inhibitory effects of the novel synthesized NHCs were compared to acetazolamide as a clinical CA isoenzymes inhibitor and tacrine as a clinical cholinergic enzymes inhibitor.
[Mh] Termos MeSH primário: Inibidores da Anidrase Carbônica/farmacologia
Inibidores da Colinesterase/farmacologia
Compostos Heterocíclicos/farmacologia
Imidazolidinas/farmacologia
Metano/análogos & derivados
[Mh] Termos MeSH secundário: Acetilcolinesterase/metabolismo
Anidrase Carbônica I/antagonistas & inibidores
Anidrase Carbônica I/metabolismo
Anidrase Carbônica II/antagonistas & inibidores
Anidrase Carbônica II/metabolismo
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Inibidores da Colinesterase/síntese química
Inibidores da Colinesterase/química
Relação Dose-Resposta a Droga
Compostos Heterocíclicos/síntese química
Compostos Heterocíclicos/química
Seres Humanos
Imidazolidinas/síntese química
Imidazolidinas/química
Ligantes
Metano/síntese química
Metano/química
Metano/farmacologia
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Cholinesterase Inhibitors); 0 (Heterocyclic Compounds); 0 (Imidazolidines); 0 (Ligands); 2465-56-7 (carbene); EC 3.1.1.7 (Acetylcholinesterase); EC 4.2.1.- (Carbonic Anhydrase I); EC 4.2.1.- (Carbonic Anhydrase II); OP0UW79H66 (Methane)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171201
[Lr] Data última revisão:
171201
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE
[do] DOI:10.1002/ardp.201700045


  10 / 9311 MEDLINE  
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[PMID]:28873528
[Au] Autor:Zeng M; Wang J; Zhang M; Chen J; He Z; Qin F; Xu Z; Cao D; Chen J
[Ad] Endereço:State Key Laboratory of Food Science and Technology, Jiangnan University, 214122 Wuxi, China. Electronic address: mmzeng@jiangnan.edu.cn.
[Ti] Título:Inhibitory effects of Sichuan pepper (Zanthoxylum bungeanum) and sanshoamide extract on heterocyclic amine formation in grilled ground beef patties.
[So] Source:Food Chem;239:111-118, 2018 Jan 15.
[Is] ISSN:0308-8146
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:This study evaluated the inhibitory effects of Sichuan pepper (Zanthoxylum bungeanum) and sanshoamide extract on the formation of heterocyclic amines (HAs) in grilled beef patties. The following major HAs were detected and quantified: imidazopyridine (2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine, PhIP), imidazoquinoxalines (2-amino-3-methyl-3H-imidazo[4,5-f]quinoxaline, IQx; 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline, MeIOx; 2-amino-3,4,8-trimethyl-3H-imidazo[4,5-f]quinoxaline, 4,8-DiMeIQx) and ß-carbolines (9H-pyrido[3,4-b]indole, norharman; 1-methyl-9H-pyrido[3,4-b]indole, harman). The rates of PhIP, IQx, MeIQx and 4,8-DiMeIQx were inhibited significantly by 82%, 61%, 28% and 79%, respectively, in patties treated with a low-concentration of pepper (0.5%), and by 27%, 45%, 44% and 26%, respectively, following treatment with a low-concentration sanshoamide extract (0.005%). All inhibition rates exceeded 70% at pepper and sanshoamide extract concentrations of 1.0% and 0.010%, respectively. Harman and norharman could be significantly (p<0.05) enhanced by the addition of all concentrations of Sichuan pepper, however, sanshoamide extract had no significant (p>0.05) effect on them, although 0.005% of the extract could slightly increase the formation of them. Notably, significant correlations were observed between the HA inhibition rates and pepper or sanshoamide extract concentrations, especially for PhIP (r=0.87, p=2.30E-3), IQx (r=0.99, p=5.04E-7) and 4,8-DiMeIQx (r=0.88, p=1.96E-3). These results indicate that Sichuan pepper and sanshoamide extract could inhibit the formation of carcinogenic HAs during thermal preparation of protein-rich foods, and therefore might reduce the risk of chronic diseases associated with the long-term intake of HA-containing food products.
[Mh] Termos MeSH primário: Carne Vermelha
[Mh] Termos MeSH secundário: Aminas
Animais
Bovinos
Culinária
Compostos Heterocíclicos
Quinoxalinas
Zanthoxylum
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Heterocyclic Compounds); 0 (Quinoxalines)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171128
[Lr] Data última revisão:
171128
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170907
[St] Status:MEDLINE



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