Base de dados : MEDLINE
Pesquisa : G02.111.570 [Categoria DeCS]
Referências encontradas : 167452 [refinar]
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[PMID]:29482394
[Au] Autor:Marcinkowska M; Kotanska M; Zagórska A; Sniecikowska J; Kubacka M; Siwek A; Bucki A; Pawlowski M; Bednarski M; Sapa J; Starek M; Dabrowska M; Kolaczkowski M
[Ad] Endereço:a Department of Medicinal Chemistry , Jagiellonian University Medical College , Kraków , Poland.
[Ti] Título:Synthesis and biological evaluation of N-arylpiperazine derivatives of 4,4-dimethylisoquinoline-1,3(2H,4H)-dione as potential antiplatelet agents.
[So] Source:J Enzyme Inhib Med Chem;33(1):536-545, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Despite the substantial clinical success of aspirin and clopidogrel in secondary prevention of ischemic stroke, up to 40% of patients remain resistant to the available antiplatelet treatment. Therefore, there is an urgent clinical need to develop novel antiplatelet agents with a novel mechanism of action. Recent studies revealed that potent alpha 2B-adrenergic receptor (alpha 2B-ARs) antagonists could constitute alternative antiplatelet therapy. We have synthesized a series of N-arylpiperazine derivatives of 4,4-dimethylisoquinoline-1,3(2H,4H)-dione as potential alpha 2B receptor antagonists. The most potent compound 3, effectively inhibited the platelet-aggregation induced both by collagen and ADP/adrenaline with IC of 26.9 µM and 20.5 µM respectively. Our study confirmed that the alpha 2B-AR antagonists remain an interesting target for the development of novel antiplatelet agents with an alternative mechanism of action.
[Mh] Termos MeSH primário: Isoquinolinas/farmacologia
Piperazinas/farmacologia
Inibidores da Agregação de Plaquetas/farmacologia
Receptores Adrenérgicos alfa 2/metabolismo
[Mh] Termos MeSH secundário: Relação Dose-Resposta a Droga
Seres Humanos
Isoquinolinas/síntese química
Isoquinolinas/química
Modelos Moleculares
Estrutura Molecular
Piperazinas/síntese química
Piperazinas/química
Agregação Plaquetária/efeitos dos fármacos
Inibidores da Agregação de Plaquetas/síntese química
Inibidores da Agregação de Plaquetas/química
Testes de Função Plaquetária
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ADRA2B protein, human); 0 (Isoquinolines); 0 (Piperazines); 0 (Platelet Aggregation Inhibitors); 0 (Receptors, Adrenergic, alpha-2); 1RTM4PAL0V (piperazine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180228
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2018.1437155


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[PMID]:29482389
[Au] Autor:Elzahabi HSA; Nossier ES; Khalifa NM; Alasfoury RA; El-Manawaty MA
[Ad] Endereço:a Department of Pharmaceutical Chemistry , Faculty of Pharmacy (Girls), Al-Azhar University , Cairo , Egypt.
[Ti] Título:Anticancer evaluation and molecular modeling of multi-targeted kinase inhibitors based pyrido[2,3-d]pyrimidine scaffold.
[So] Source:J Enzyme Inhib Med Chem;33(1):546-557, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:An efficient synthesis of substituted pyrido[2,3-d]pyrimidines was carried out and evaluated for in vitro anticancer activity against five cancer cell lines, namely hepatic cancer (HepG-2), prostate cancer (PC-3), colon cancer (HCT-116), breast cancer (MCF-7), and lung cancer (A-549) cell lines. Regarding HepG-2, PC-3, HCT-116 cancer cell lines, 7-(4-chlorophenyl)-2-(3-methyl-5-oxo-2,3-dihydro-1H-pyrazol-1-yl)-5-(p-tolyl)- pyrido[2,3-d]pyrimidin-4(3H)-one (5a) exhibited strong, more potent anticancer (IC : 0.3, 6.6 and 7 µM) relative to the standard doxorubicin (IC : 0.6, 6.8 and 12.8 µM), respectively. Kinase inhibitory assessment of 5a showed promising inhibitory activity against three kinases namely PDGFR ß, EGFR, and CDK4/cyclin D1 at two concentrations 50 and 100 µM in single measurements. Further, a molecular docking study for compound 5a was performed to verify the binding mode towards the EGFR and CDK4/cyclin D1 kinases.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Quinase 4 Dependente de Ciclina/antagonistas & inibidores
Inibidores de Proteínas Quinases/farmacologia
Piridinas/farmacologia
Pirimidinas/farmacologia
Receptor do Fator de Crescimento Epidérmico/antagonistas & inibidores
Receptor beta de Fator de Crescimento Derivado de Plaquetas/antagonistas & inibidores
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Quinase 4 Dependente de Ciclina/metabolismo
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Modelos Moleculares
Estrutura Molecular
Inibidores de Proteínas Quinases/síntese química
Inibidores de Proteínas Quinases/química
Piridinas/síntese química
Piridinas/química
Pirimidinas/síntese química
Pirimidinas/química
Receptor do Fator de Crescimento Epidérmico/metabolismo
Receptor beta de Fator de Crescimento Derivado de Plaquetas/metabolismo
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Protein Kinase Inhibitors); 0 (Pyridines); 0 (Pyrimidines); 0 (pyrido(3,2-d)pyrimidine); EC 2.7.10.1 (Receptor, Epidermal Growth Factor); EC 2.7.10.1 (Receptor, Platelet-Derived Growth Factor beta); EC 2.7.11.22 (CDK4 protein, human); EC 2.7.11.22 (Cyclin-Dependent Kinase 4)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180228
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2018.1437729


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[PMID]:29185703
[Au] Autor:Hoffmann M; Auerbach D; Panter F; Hoffmann T; Dorrestein PC; Müller R
[Ad] Endereço:Department of Microbial Natural Products (MINS), Department of Microbial Natural Products (MINS), Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) - Helmholtz Centre for Infection Research (HZI) and Institute for Pharmaceutical Biotechnology, Saarland University , 66123 Saarbrücken, G
[Ti] Título:Homospermidine Lipids: A Compound Class Specifically Formed during Fruiting Body Formation of Myxococcus xanthus DK1622.
[So] Source:ACS Chem Biol;13(1):273-280, 2018 01 19.
[Is] ISSN:1554-8937
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The fascinating ability of myxobacteria to form multicellular spore filled fruiting bodies under starvation conditions was widely studied as a model for cooperative microbial behavior. The potential of a life cycle induced change of secondary metabolism, as a means to discover novel natural products, remains largely underexplored. We therefore studied the model organism Myxococcus xanthus DK1622 under submersed and solid cultivation conditions to find putatively life-cycle related compounds by applying statistical analysis on analytical data. Utilizing the advantageous characteristics of LC-MS, LC-MS/MS, and MALDI-MSI allowed the identification of compounds unambiguously associated with myxobacterial fruiting bodies. Our screening effort resulted in the purification and structure elucidation of a novel compound, the homospermidine lipid, from cultures that had undergone the fruiting process. A combination of molecular networking and targeted LC-MS/MS in conjunction with our in-house metabolomics database subsequently revealed alternative producers of the respective compound as well as a number of compounds belonging to the same structural class. Three further members of this compound class were isolated from an alternative producer and structurally elucidated by NMR. Insights into the biosynthesis of this novel compound class was gained by feeding of isotopically labeled substrates and in silico analysis.
[Mh] Termos MeSH primário: Lipídeos/química
Myxococcus xanthus/metabolismo
Espermidina/metabolismo
[Mh] Termos MeSH secundário: Estrutura Molecular
Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Lipids); U87FK77H25 (Spermidine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171130
[St] Status:MEDLINE
[do] DOI:10.1021/acschembio.7b00816


  4 / 167452 MEDLINE  
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[PMID]:29175397
[Au] Autor:Dong G; Huang L; Wu X; Wang C; Liu Y; Liu G; Wang L; Liu X; Xia H
[Ad] Endereço:Shandong Key Laboratory of Water Pollution Control and Resource Reuse, School of Environmental Science and Engineering, Shandong University, Jinan, 250100, China. Electronic address: 963722867@qq.com.
[Ti] Título:Effect and mechanism analysis of MnO on permeable reactive barrier (PRB) system for the removal of tetracycline.
[So] Source:Chemosphere;193:702-710, 2018 Feb.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Effect of manganese dioxide (MnO ) on tetracycline (TC) removal/degradation in zero-valent iron (ZVI) based permeable reactive barrier (PRB) system was investigated. To analyze the role of MnO , three different PRB columns packed with ZVI, ZVI and a layer of MnO , and MnO were set up to investigate the removal effect and reaction mechanism of ZVI coupling with MnO on TC removal, respectively. The results show that the removal efficiencies of three PRB columns are 65%, 85%, and 50%, respectively. MnO could accelerate the transformation of Fe into Fe and combine with Fe to degrade TC in different reaction sites in the ZVI-MnO PRB system. Hydroxyl radicals (·OH) were produced in this process, which contributed to about 58.3% for the TC degradation. The UV-Vis spectrum demonstrated that A ring of TC was the main reaction site for interaction with Fe and the BCD rings were crucial for interactions with MnO . On the basis of intermediates identified by LC-ESI-MS, the ring structure of TC was opened, and low-molecular-weight compounds were produced in ZVI-MnO PRB system.
[Mh] Termos MeSH primário: Ferro/química
Compostos de Manganês/farmacologia
Óxidos/farmacologia
Tetraciclina/isolamento & purificação
[Mh] Termos MeSH secundário: Sítios de Ligação
Cromatografia Líquida
Estrutura Molecular
Espectrometria de Massas em Tandem
Tetraciclina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Manganese Compounds); 0 (Oxides); E1UOL152H7 (Iron); F8VB5M810T (Tetracycline); TF219GU161 (manganese dioxide)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE


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[PMID]:28888123
[Au] Autor:Tot A; Vranes M; Maksimovic I; Putnik-Delic M; Danicic M; Belic S; Gadzuric S
[Ad] Endereço:University of Novi Sad, Faculty of Sciences, Department of Chemistry, Biochemistry and Environmental Protection, Trg D. Obradovica 3, 21000 Novi Sad, Serbia.
[Ti] Título:The effect of imidazolium based ionic liquids on wheat and barley germination and growth: Influence of length and oxygen functionalization of alkyl side chain.
[So] Source:Ecotoxicol Environ Saf;147:401-406, 2018 Jan.
[Is] ISSN:1090-2414
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In this work five different imidazolium based ionic liquids, namely: 1-(2-oxybutyl)-3-methylimidazolium chloride, [C OC mIm][Cl]; 1-(2-oxypropyl)-3-methylimidazolium chloride, [C OC mIm][Cl]; 1-(3-hydroxypropyl)-3-ethylimidazolium chloride, [OHC eIm][Cl]; 1-(3-hydroxypropyl)-3-methylimidazolium chloride, [OHC mIm][Cl]; 1-(2-hydroxyethyl)-3-methylimidazolium chloride, [OHC mIm][Cl], together with commercial 1-butyl-3-methylimidazolium chloride, [bmim][Cl] and synthesized protic imidazolium chloride, [Im][Cl], were prepared and their toxicity examined towards wheat and barley germination and growth. Introduction of the polar groups (in the form of hydroxyde and/or ether group) in the alkyl side chain of the imidazolium cation and their influence on the reduction of the ionic liquid's toxicity is demonstrated. The results indicate that toxicity of oxygen functionalized ILs is significantly lower against wheat comparing to non-functionalized analogues. In the case of barley, influence on germination follow the same trend as in the case of wheat, but for seedlings growth different trend is observed with more pronounced toxicity of ether functionalized ILs. From these results it was also shown that alkylation in the position N-3 atom of the imidazole significantly reduces toxicity of cation.
[Mh] Termos MeSH primário: Germinação/efeitos dos fármacos
Hordeum/efeitos dos fármacos
Imidazóis/toxicidade
Líquidos Iônicos/toxicidade
Oxigênio/química
Triticum/efeitos dos fármacos
[Mh] Termos MeSH secundário: Cátions
Hordeum/crescimento & desenvolvimento
Imidazóis/síntese química
Imidazóis/química
Líquidos Iônicos/síntese química
Líquidos Iônicos/química
Estrutura Molecular
Plântulas/efeitos dos fármacos
Plântulas/crescimento & desenvolvimento
Triticum/crescimento & desenvolvimento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cations); 0 (Imidazoles); 0 (Ionic Liquids); 41PS77334A (1-butyl-3-methylimidazolium chloride); 7GBN705NH1 (imidazole); S88TT14065 (Oxygen)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170910
[St] Status:MEDLINE


  6 / 167452 MEDLINE  
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[PMID]:28453010
[Au] Autor:Sethi S; Ooe M; Sakamoto T; Fujimoto K
[Ad] Endereço:School of Materials Science, Japan Advanced Institute of Science and Technology, 1-1 Asahidai, Nomi, Ishikawa 923-1292, Japan. kenzo@jaist.ac.jp.
[Ti] Título:Effect of nucleobase change on cytosine deamination through DNA photo-cross-linking reaction via 3-cyanovinylcarbazole nucleoside.
[So] Source:Mol Biosyst;13(6):1152-1156, 2017 Jun 01.
[Is] ISSN:1742-2051
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Photo-chemical deamination of cytosine using 3-cyanovinylcarbazole nucleoside ( K) mediated photo-cross-linking is a technique for site-directed mutagenesis. Using this technique in vivo requires the elimination of a high-temperature incubation step; instead, incubation should be carried out under physiological conditions. To improve the reactivity of K mediated photo-cross-link induced deamination of cytosine under physiological conditions, an evaluation of base pairing in cytosine was carried out with respect to its deamination. Guanine was replaced with 4 different counter bases (inosine, 2-aminopurine, 5-nitroindole, and nebularine), showing distinct hydrogen bonding patterns with target cytosine, which was incorporated at the -1 position with respect to K in the K-modified photo-responsive oligodeoxyribonucleotides to ascertain the role of hydrogen bonding in deamination under physiological conditions. Among the counter bases, inosine showed the highest acceleration towards the photo-induced deamination reaction.
[Mh] Termos MeSH primário: Citosina/química
DNA/química
Guanina/química
Nucleosídeos/química
[Mh] Termos MeSH secundário: 2-Aminopurina/química
Pareamento de Bases
Desaminação
Ligações de Hidrogênio
Indóis/química
Estrutura Molecular
Mutagênese Sítio-Dirigida
Oligodesoxirribonucleotídeos/química
Nucleosídeos de Purina/química
Ribonucleosídeos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Indoles); 0 (Nucleosides); 0 (Oligodeoxyribonucleotides); 0 (Purine Nucleosides); 0 (Ribonucleosides); 452-06-2 (2-Aminopurine); 5Z93L87A1R (Guanine); 8J337D1HZY (Cytosine); 9007-49-2 (DNA); B8B604PS4P (nebularine); O2BHX6EDBN (5-nitroindole)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170429
[St] Status:MEDLINE
[do] DOI:10.1039/c7mb00082k


  7 / 167452 MEDLINE  
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[PMID]:28452222
[Au] Autor:Zhu Y; Serra A; Guo T; Park JE; Zhong Q; Sze SK
[Ad] Endereço:School of Biological Sciences, Nanyang Technological University , 60 Nanyang Drive 637551, Singapore.
[Ti] Título:Application of Nanosecond Laser Photolysis Protein Footprinting to Study EGFR Activation by EGF in Cells.
[So] Source:J Proteome Res;16(6):2282-2293, 2017 Jun 02.
[Is] ISSN:1535-3907
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Mass spectrometry-based protein footprinting emerged as a useful technology to understand protein ligand interactions in vitro. We have previously demonstrated the application of footprinting in live E. coli cells. Here, we further optimized an ultrafast laser photolysis hydroxyl radical footprinting method and applied it to study the interaction of EGF and EGFR in live mammalian cells. This method used a nanosecond laser to photochemically generate a burst of hydroxyl radicals in situ in-cell suspension to oxidize the amino acids on the protein surface. Mass spectrometric analysis of the thus modified peptides was interpreted to probe the solvent-accessible surface areas of the protein in its native biological state with and without EGF activation. Our footprinting data agreed with the two relevant EGFR crystal structures, indicating that this in-cell laser photolysis footprinting technique is a valid approach to study the structural properties of integral membrane proteins directly in the native environment.
[Mh] Termos MeSH primário: Fator de Crescimento Epidérmico/metabolismo
Pegadas de Proteínas/métodos
Receptor do Fator de Crescimento Epidérmico/metabolismo
[Mh] Termos MeSH secundário: Aminoácidos/química
Ativação Enzimática
Células HEK293
Seres Humanos
Radical Hidroxila
Lasers
Proteínas de Membrana/metabolismo
Estrutura Molecular
Oxirredução
Fotólise
Receptor do Fator de Crescimento Epidérmico/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Amino Acids); 0 (Membrane Proteins); 3352-57-6 (Hydroxyl Radical); 62229-50-9 (Epidermal Growth Factor); EC 2.7.10.1 (EGFR protein, human); EC 2.7.10.1 (Receptor, Epidermal Growth Factor)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170429
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jproteome.7b00154


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[PMID]:29357800
[Au] Autor:Siverio-Mota D; Andujar I; Marrero-Ponce Y; Giner RM; Diaz-Mendoza C; Paba GM; Vicet-Muro L; Cordero-Maldonado ML; de Witte PAM; Crawford AD; Veitia MS; Perez-Jimenez F; Aran VJ
[Ad] Endereço:Laboratory for Molecular Biodiscovery, Department of Pharmaceutical and Pharmacological Sciences, University of Leuven, Herestraat 49, 3000 Leuven, Belgium.
[Ti] Título:Anti-Inflammatory Activity and Cheminformatics Analysis of New Poten t 2-Substituted 1-Methyl-5-Nitroindazolinones.
[So] Source:Curr Top Med Chem;17(30):3236-3248, 2018 Feb 09.
[Is] ISSN:1873-4294
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:After the identification of the anti-inflammatory properties of VA5-13l (2-benzyl-1- methyl-5-nitroindazolinone) in previous investigations, some of its analogous compounds were designed, synthesized and evaluated in two anti-inflammatory methods: LPS-enhanced leukocyte migration assay in zebrafish; and 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema. The products evaluated (3, 6, 8, 9 and 10) showed the lower values of relative leukocyte migration at 30 µM (0.14, 0.07, 0.10, 0.13 and 0.07, respectively), while in ear edema and myeloperoxidase activity methods, all the compounds reduced inflammation, only 4 and 16 yielded unsatisfactory results. The relationship linking structure and activity (SAR analysis) was determinate by using SARANEA software. The importance of the 5-Nitro group of the indazole ring for the activity was evident, and showed modest reduction when benzyl (Bn) is changed by alkyl group. A substituted Bn moiety at N2 (R) is the best substituent (5-10); nevertheless, if methylene group of Bn is deleted, the activity is affected. Also, introduction of halogen atoms mainly at positions 3 or 4 of the benzyl moiety (6 and 10) leads in general to strong activities. In fact, compounds 7 and 8 (R = 4-FBn or 4-ClBn, respectively) exhibit satisfactory results in in vivo tests and appear promising. The production of IL-6 at all doses assayed was significantly reduced, except with 16. Nonetheless, the production of TNF-α was significantly inhibited only by this chemical (16) at concentration of 50 µM. On the other hand, compound 2 was the one that mostly inhibited the expression of COX-2 and iNOS. From these results, it can be concluded that the inhibition in the release of cytokines can be one of the mechanisms of action responsible for the anti-inflammatory effect for 2-benzyl derivates while other 2-alkyl derivatives can inhibit production of NO. Therefore, nitroindazolinone chemical prototype could be an interesting structural group with anti-inflammatory purposes in the therapeutic.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/farmacologia
Inibidores de Ciclo-Oxigenase 2/farmacologia
Indazóis/farmacologia
Informática
Nitrocompostos/farmacologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides/química
Ciclo-Oxigenase 2/metabolismo
Inibidores de Ciclo-Oxigenase 2/química
Relação Dose-Resposta a Droga
Seres Humanos
Indazóis/química
Lipopolissacarídeos/antagonistas & inibidores
Lipopolissacarídeos/farmacologia
Estrutura Molecular
Óxido Nítrico/antagonistas & inibidores
Óxido Nítrico/biossíntese
Óxido Nítrico Sintase Tipo II/antagonistas & inibidores
Óxido Nítrico Sintase Tipo II/metabolismo
Nitrocompostos/química
Relação Estrutura-Atividade
Fator de Necrose Tumoral alfa/antagonistas & inibidores
Peixe-Zebra
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Cyclooxygenase 2 Inhibitors); 0 (Indazoles); 0 (Lipopolysaccharides); 0 (Nitro Compounds); 0 (Tumor Necrosis Factor-alpha); 31C4KY9ESH (Nitric Oxide); EC 1.14.13.39 (Nitric Oxide Synthase Type II); EC 1.14.99.1 (Cyclooxygenase 2)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180124
[St] Status:MEDLINE
[do] DOI:10.2174/1568026618666180119125255


  9 / 167452 MEDLINE  
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Texto completo SciELO Brasil
[PMID]:29267507
[Au] Autor:Liu N; Ding D; Wang L; Zhao H; Zhu L; Geng X
[Ad] Endereço:Department of Critical Care Medicine, The First Affiliated Hospital of Anhui Medical University, Hefei, Anhui, China.
[Ti] Título:Two novel Mg(II)-based and Zn(II)-based complexes: inhibiting growth of human liver cancer cells.
[So] Source:Braz J Med Biol Res;51(2):e6929, 2017 Dec 18.
[Is] ISSN:1414-431X
[Cp] País de publicação:Brazil
[La] Idioma:eng
[Ab] Resumo:Two new Mg(II)-based and Zn(II)-based coordination polymers, {[Mg3(BTB)(DMA)4](DMA)2}n (1, H3BTB=1,3,5-benzenetrisbenzoic acid, DMA=N,N-dimethylacetamide) and {(H2NMe2)2[Zn3(BTB)2(OH)(Im)](DMF)9(MeOH)7}n (2, Im=imidazole, DMF=N,N-dimethylformamide), have been successfully synthesized and structurally characterized under solvothermal conditions. 1 contains a linear [Mg3(COO)6] cluster that connected by the fully deprotonated BTB3- ligands to give a kgd-type 2D bilayer structure; 2 represents a microporous 3D pillar-layered system based on the binuclear Zn units and pillared Im ligands, which shows a (3,5)-connected hms topological net. In addition, in vitro anticancer activities of compounds 1 and 2 on 4 human liver cancer cells (HB611, HHCC, BEL-7405 and SMMC-7721) were determined.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Benzimidazóis/farmacologia
Neoplasias Hepáticas/tratamento farmacológico
Estruturas Metalorgânicas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Benzimidazóis/síntese química
Linhagem Celular Tumoral
Seres Humanos
Ligantes
Neoplasias Hepáticas/patologia
Magnésio/química
Estruturas Metalorgânicas/síntese química
Estrutura Molecular
Zinco/química
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Benzimidazoles); 0 (Ligands); 0 (Metal-Organic Frameworks); I38ZP9992A (Magnesium); J41CSQ7QDS (Zinc)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171222
[St] Status:MEDLINE


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[PMID]:29231144
[Au] Autor:Castellano G; Redondo L; Torrens F
[Ad] Endereço:Departamento de Ciencias Experimentales y Matematicas, Facultad de Veterinaria y Ciencias Experimentales, Universidad Catolica de Valencia San Vicente Martir, Guillem de Castro-94, E-46001 Valencia, Spain.
[Ti] Título:QSAR of Natural Sesquiterpene Lactones as Inhibitors of Myb-dependent Gene Expression.
[So] Source:Curr Top Med Chem;17(30):3256-3268, 2018 Feb 09.
[Is] ISSN:1873-4294
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Protein c-Myb is a therapeutic target. Some sesquiterpene lactones suppress Myb-dependent gene expression, which results in their potential anti-cancer activity. MATERIAL & METHODS: Database ChEMBL is a representative of lactones for physicochemical and physiochemical properties. Data presented for 31 natural lactones are discussed in terms of quantitative structureactivity relationships with the objective to predict inhibitors of Myb-induced gene expression. Several constitutional descriptors are related to structure-activity. α-Methylene-γ-lactone groups enhance while OH functions worsen potency. The latter feature is in agreement with the fact that the more lipophilic the lactone, the greater the cytotoxicity because of the ability to cross lipoidal biomembranes. In general, numbers of π-systems and atoms, and polarizability enhance activity. Linear and nonlinear structure-activity models are developed, between lactones of a great structural diversity, to predict inhibitors of Myb-induced gene expression. Four variables (ML, UNC, TCO+OCOR, UNC+UNA) related to ATOM show a positive correlation because of the partial anionic and H-acceptor characters of O-atom. In most, CO group is conjugated. RESULT AND CONCLUSION: Term OH shows negative coefficients because of the partial cationic quality of H-atom and because OH forms H-bonds with CO, causing them to be less H-acceptor. s-trans-s-trans-Germacranolide structure is the most active. Coefficients standard errors result acceptable in almost all equations. After cross-validation, linear equations for lactones, pseudoguaianolides and germacranolides are the most predictive. Most descriptors are constitutional variables.
[Mh] Termos MeSH primário: Produtos Biológicos/farmacologia
Regulação da Expressão Gênica/efeitos dos fármacos
Lactonas/farmacologia
Proteínas Proto-Oncogênicas c-myb/antagonistas & inibidores
Relação Quantitativa Estrutura-Atividade
Sesquiterpenos/farmacologia
[Mh] Termos MeSH secundário: Produtos Biológicos/química
Relação Dose-Resposta a Droga
Seres Humanos
Lactonas/química
Modelos Moleculares
Estrutura Molecular
Proteínas Proto-Oncogênicas c-myb/genética
Sesquiterpenos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biological Products); 0 (Lactones); 0 (Proto-Oncogene Proteins c-myb); 0 (Sesquiterpenes)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171213
[St] Status:MEDLINE
[do] DOI:10.2174/1568026618666171211145846



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