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  1 / 231404 MEDLINE  
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[PMID]:28452485
[Au] Autor:Li H; Park J; Kim H; Hwang KB; Paek E
[Ad] Endereço:School of Computer Science and Engineering, Soongsil University , Seoul 06978, Republic of Korea.
[Ti] Título:Systematic Comparison of False-Discovery-Rate-Controlling Strategies for Proteogenomic Search Using Spike-in Experiments.
[So] Source:J Proteome Res;16(6):2231-2239, 2017 Jun 02.
[Is] ISSN:1535-3907
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Proteogenomic searches are useful for novel peptide identification from tandem mass spectra. Usually, separate and multistage approaches are adopted to accurately control the false discovery rate (FDR) for proteogenomic search. Their performance on novel peptide identification has not been thoroughly evaluated, however, mainly due to the difficulty in confirming the existence of identified novel peptides. We simulated a proteogenomic search using a controlled, spike-in proteomic data set. After confirming that the results of the simulated proteogenomic search were similar to those of a real proteogenomic search using a human cell line data set, we evaluated the performance of six FDR control methods-global, separate, and multistage FDR estimation, respectively, coupled to a target-decoy search and a mixture model-based method-on novel peptide identification. The multistage approach showed the highest accuracy for FDR estimation. However, global and separate FDR estimation with the mixture model-based method showed higher sensitivities than others at the same true FDR. Furthermore, the mixture model-based method performed equally well when applied without or with a reduced set of decoy sequences. Considering different prior probabilities for novel and known protein identification, we recommend using mixture model-based methods with separate FDR estimation for sensitive and reliable identification of novel peptides from proteogenomic searches.
[Mh] Termos MeSH primário: Peptídeos/análise
Proteogenômica/métodos
[Mh] Termos MeSH secundário: Linhagem Celular
Simulação por Computador
Reações Falso-Positivas
Seres Humanos
Métodos
Modelos Teóricos
Espectrometria de Massas em Tandem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Peptides)
[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.7b00033


  2 / 231404 MEDLINE  
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[PMID]:28985541
[Au] Autor:Wang W
[Ad] Endereço:College of Chemistry and Chemical Engineering, Dezhou University, Dezhou 253023, China. Electronic address: wwqzs@126.com.
[Ti] Título:Chromium (â…¥) removal from aqueous solutions through powdered activated carbon countercurrent two-stage adsorption.
[So] Source:Chemosphere;190:97-102, 2018 Jan.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:To exploit the adsorption capacity of commercial powdered activated carbon (PAC) and to improve the efficiency of Cr(VI) removal from aqueous solutions, the adsorption of Cr(VI) by commercial PAC and the countercurrent two-stage adsorption (CTA) process was investigated. Different adsorption kinetics models and isotherms were compared, and the pseudo-second-order model and the Langmuir and Freundlich models fit the experimental data well. The Cr(VI) removal efficiency was >80% and was improved by 37% through the CTA process compared with the conventional single-stage adsorption process when the initial Cr(VI) concentration was 50 mg/L with a PAC dose of 1.250 g/L and a pH of 3. A calculation method for calculating the effluent Cr(VI) concentration and the PAC dose was developed for the CTA process, and the validity of the method was confirmed by a deviation of <5%.
[Mh] Termos MeSH primário: Adsorção
Cromo/isolamento & purificação
Purificação da Água/métodos
[Mh] Termos MeSH secundário: Carcinógenos Ambientais
Carvão Vegetal/química
Cinética
Métodos
Poluentes Químicos da Água/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Carcinogens, Environmental); 0 (Water Pollutants, Chemical); 0R0008Q3JB (Chromium); 16291-96-6 (Charcoal); 18540-29-9 (chromium hexavalent ion)
[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:171007
[St] Status:MEDLINE


  3 / 231404 MEDLINE  
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[PMID]:29024883
[Au] Autor:Sopilniak A; Elkayam R; Rossin AV; Lev O
[Ad] Endereço:Casali Center of Applied Chemistry, The Institute of Chemistry, The Hebrew University of Jerusalem, Jerusalem 9190401, Israel.
[Ti] Título:Emerging organic pollutants in the vadose zone of a soil aquifer treatment system: Pore water extraction using positive displacement.
[So] Source:Chemosphere;190:383-392, 2018 Jan.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Trace organic compounds in effluents, water streams and aquifers are amply reported. However, the mobile pool of Emerging Organic Contaminants (EOCs) in the deep parts of the vadose zone is hard to estimate, due to difficulties in extraction of sufficient quantity of pore water. Here, we present a new methodology for depth profiling of EOCs in pore water by Positive Displacement Extraction (PDE): Pore water extraction from unsaturated soil samples is carried out by withdrawal of soil cores by direct-push drilling and infiltrating the core by organics free water. We show that EOC concentrations in the water eluted in the plateau region of the inverse breakthrough curve is equal to their pore water concentrations. The method was previously validated for DOC extraction, and here the scope of the methodology is extended to pore water extraction for organic pollutants analysis. Method characteristics and validation were carried out with atrazine, simazine, carbamazepine, venlafaxine, O-desmethylvenlafaxine and caffeine in the concentration range of several ng to several µg/liter. Validation was carried out by laboratory experiments on three different soils (sandy, sandy-clayey and clayey). Field studies in the vadose zone of a SAT system provided 27 m deep EOC profiles with less than 1.5 m spatial resolution. During the percolation treatment, carbamazepine remained persistent, while the other studied EOCs were attenuated to the extent of 50-99%.The highest degradation rate of all studied EOCs was in the aerobic zone. EOC levels based on PDE and extraction by centrifugation were compared, showing a positive bias for centrifugation.
[Mh] Termos MeSH primário: Água Subterrânea/análise
Poluentes do Solo/análise
Extração em Fase Sólida/métodos
Poluentes Químicos da Água/análise
[Mh] Termos MeSH secundário: Atrazina/análise
Carbamazepina/análise
Succinato de Desvenlafaxina/análise
Métodos
Compostos Orgânicos/análise
Simazina
Solo/química
Água/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Organic Chemicals); 0 (Soil); 0 (Soil Pollutants); 0 (Water Pollutants, Chemical); 059QF0KO0R (Water); 33CM23913M (Carbamazepine); QJA9M5H4IM (Atrazine); SG0C34SMY3 (Simazine); ZB22ENF0XR (Desvenlafaxine Succinate)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180228
[Lr] Data última revisão:
180228
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171013
[St] Status:MEDLINE


  4 / 231404 MEDLINE  
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[PMID]:29320540
[Au] Autor:Rockett IRH; Caine ED; Connery HS; D'Onofrio G; Gunnell DJ; Miller TR; Nolte KB; Kaplan MS; Kapusta ND; Lilly CL; Nelson LS; Putnam SL; Stack S; Värnik P; Webster LR; Jia H
[Ad] Endereço:Department of Epidemiology, West Virginia University, Morgantown, West Virginia, United States of America.
[Ti] Título:Discerning suicide in drug intoxication deaths: Paucity and primacy of suicide notes and psychiatric history.
[So] Source:PLoS One;13(1):e0190200, 2018.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: A paucity of corroborative psychological and psychiatric evidence may be inhibiting detection of drug intoxication suicides in the United States. We evaluated the relative importance of suicide notes and psychiatric history in the classification of suicide by drug intoxication versus firearm (gunshot wound) plus hanging/suffocation-the other two major, but overtly violent methods. METHODS: This observational multilevel (individual/county), multivariable study employed a generalized linear mixed model (GLMM) to analyze pooled suicides and undetermined intent deaths, as possible suicides, among the population aged 15 years and older in the 17 states participating in the National Violent Death Reporting System throughout 2011-2013. The outcome measure was relative odds of suicide versus undetermined classification, adjusted for demographics, precipitating circumstances, and investigation characteristics. RESULTS: A suicide note, prior suicide attempt, or affective disorder was documented in less than one-third of suicides and one-quarter of undetermined deaths. The prevalence gaps were larger among drug intoxication cases than gunshot/hanging cases. The latter were more likely than intoxication cases to be classified as suicide versus undetermined manner of death (adjusted odds ratio [OR], 41.14; 95% CI, 34.43-49.15), as were cases documenting a suicide note (OR, 33.90; 95% CI, 26.11-44.05), prior suicide attempt (OR, 2.42; 95% CI, 2.11-2.77), or depression (OR, 1.61; 95% CI, 1.38 to 1.88), or bipolar disorder (OR, 1.41; 95% CI, 1.10-1.81). Stratification by mechanism/cause intensified the association between a note and suicide classification for intoxication cases (OR, 45.43; 95% CI, 31.06-66.58). Prior suicide attempt (OR, 2.64; 95% CI, 2.19-3.18) and depression (OR, 1.48; 95% CI, 1.17-1.87) were associated with suicide classification in intoxication but not gunshot/hanging cases. CONCLUSIONS: Without psychological/psychiatric evidence contributing to manner of death classification, suicide by drug intoxication in the US is likely profoundly under-reported. Findings harbor adverse implications for surveillance, etiologic understanding, and prevention of suicides and drug deaths.
[Mh] Termos MeSH primário: Overdose de Drogas/psicologia
Intenção
Suicídio/psicologia
[Mh] Termos MeSH secundário: Adolescente
Adulto
Idoso
Asfixia
Causas de Morte
Depressão/epidemiologia
Feminino
Seres Humanos
Masculino
Registros Médicos
Métodos
Meia-Idade
Transtornos do Humor/epidemiologia
Vigilância da População
Recidiva
Tentativa de Suicídio
Ferimentos por Arma de Fogo
Redação
Adulto Jovem
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; MULTICENTER STUDY; OBSERVATIONAL STUDY; RESEARCH SUPPORT, NON-U.S. GOV'T
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180214
[Lr] Data última revisão:
180214
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180111
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0190200


  5 / 231404 MEDLINE  
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[PMID]:28745519
[Au] Autor:Gonçalves RS; Silva EL; Hioka N; Nakamura CV; Bruschi ML; Caetano W
[Ad] Endereço:a Department of Chemistry , State University of Maringá , Maringá , Brazil.
[Ti] Título:An optimized protocol for anthraquinones isolation from Rhamnus frangula L.
[So] Source:Nat Prod Res;32(3):366-369, 2018 Feb.
[Is] ISSN:1478-6427
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Different from works described in the literature, which use expansive analytical methods to separation of anthraquinones derivatives (AQs), this communication reported a simple and inexpensive methodology to get them. In this way, the expensive commercial AQs: Chrysophanol, physcione and emodine were extracted from plant material (Rhamnus frangula L.) and isolated by classical column chromatography technique under optimised binary mobile phase gradients (CHCl : AcOEt(a), a = 1 to 5%) in excellent yields.
[Mh] Termos MeSH primário: Antraquinonas/isolamento & purificação
Frangula/química
Rhamnus/química
[Mh] Termos MeSH secundário: Antraquinonas/análise
Cromatografia/métodos
Emodina/análogos & derivados
Emodina/análise
Emodina/isolamento & purificação
Métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anthraquinones); H6PT94IV61 (physcione); KA46RNI6HN (Emodin); N1ST8V8RR2 (chrysophanic acid)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180212
[Lr] Data última revisão:
180212
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170727
[St] Status:MEDLINE
[do] DOI:10.1080/14786419.2017.1356836


  6 / 231404 MEDLINE  
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[PMID]:29223150
[Au] Autor:Filippova JA; Semenov DV; Juravlev ES; Komissarov AB; Richter VA; Stepanov GA
[Ad] Endereço:Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences, Novosibirsk, 630090, Russia. stepanovga@niboch.nsc.ru.
[Ti] Título:Modern Approaches for Identification of Modified Nucleotides in RNA.
[So] Source:Biochemistry (Mosc);82(11):1217-1233, 2017 Nov.
[Is] ISSN:1608-3040
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:This review considers approaches for detection of modified monomers in the RNA structure of living organisms. Recently, some data on dynamic alterations in the pool of modifications of the key RNA species that depend on external factors affecting the cells and physiological conditions of the whole organism have been accumulated. The recent studies have presented experimental data on relationship between the mechanisms of formation of modified/minor nucleotides of RNA in mammalian cells and the development of various pathologies. The development of novel methods for detection of chemical modifications of RNA nucleotides in the cells of living organisms and accumulation of knowledge on the contribution of modified monomers to metabolism and functioning of individual RNA species establish the basis for creation of novel diagnostic and therapeutic approaches. This review includes a short description of routine methods for determination of modified nucleotides in RNA and considers in detail modern approaches that enable not only detection but also quantitative assessment of the modification level of various nucleotides in individual RNA species.
[Mh] Termos MeSH primário: Nucleotídeos/química
Processamento Pós-Transcricional do RNA
RNA/genética
[Mh] Termos MeSH secundário: Animais
Técnicas de Química Analítica/instrumentação
Técnicas de Química Analítica/métodos
Cromatografia Líquida de Alta Pressão
Técnicas Genéticas
Seres Humanos
Espectrometria de Massas
Métodos
Nucleotídeos/análise
Transcrição Reversa
Ribonucleases/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Nucleotides); 63231-63-0 (RNA); EC 3.1.- (Ribonucleases)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180103
[Lr] Data última revisão:
180103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171211
[St] Status:MEDLINE
[do] DOI:10.1134/S0006297917110013


  7 / 231404 MEDLINE  
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[PMID]:28906323
[Au] Autor:Degnin M; Agarwal A; Tarlock K; Meshinchi S; Druker BJ; Tognon CE
[Ad] Endereço:*Knight Cancer Institute, Oregon Health and Science University ‡Howard Hughes Medical Institute, Portland, OR †Fred Hutchinson Cancer Research Center, Seattle, WA.
[Ti] Título:Novel Method Enabling the Use of Cryopreserved Primary Acute Myeloid Leukemia Cells in Functional Drug Screens.
[So] Source:J Pediatr Hematol Oncol;39(7):e359-e366, 2017 Oct.
[Is] ISSN:1536-3678
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The ability to assess antileukemic drug activity on primary patient samples is a powerful tool in determining potential drug targets and selection of therapeutic agents with biological and functional rationale. We previously established small molecule inhibitor screens for use on freshly isolated leukemia cells for this purpose. Here we describe a method that produces functional small molecule inhibitor screening results using cryopreserved primary acute myeloid leukemia cells. This method was established to take advantage of biorepositories containing archival material, such as those established by the Children's Oncology Group, and to enable validation of potential pathway dependencies uncovered by genomic analysis. Various conditions used to thaw and culture cryopreserved specimens were assessed for effect on viability, differentiation, and the ability to recapitulate sensitivity results obtained on fresh samples. The most reproducible results were obtained by quick-thawing and culturing samples in cytokine rich media before performing drug screens. Our data suggest that cytokine-enriched media aids in maintaining the viability and numbers required to perform functional analysis on cryopreserved leukemia cells. This method can aid in producing informative data on therapeutic targeting and precision medicine efforts in leukemia by making use of biorepositories and bio banks.
[Mh] Termos MeSH primário: Criopreservação
Ensaios de Seleção de Medicamentos Antitumorais/métodos
Leucemia Mieloide Aguda/tratamento farmacológico
Leucemia Mieloide Aguda/patologia
Medicina de Precisão/métodos
[Mh] Termos MeSH secundário: Técnicas de Cultura de Células
Diferenciação Celular
Sobrevivência Celular
Meios de Cultura/normas
Seres Humanos
Métodos
Manejo de Espécimes
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Culture Media)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171025
[Lr] Data última revisão:
171025
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170915
[St] Status:MEDLINE
[do] DOI:10.1097/MPH.0000000000000946


  8 / 231404 MEDLINE  
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[PMID]:28681458
[Au] Autor:Watanabe N; Nogawa M; Ishiguro M; Maruyama H; Shiba M; Satake M; Eto K; Handa M
[Ad] Endereço:Center for Transfusion Medicine and Cell Therapy, Keio University School of Medicine.
[Ti] Título:Refined methods to evaluate the in vivo hemostatic function and viability of transfused human platelets in rabbit models.
[So] Source:Transfusion;57(8):2035-2044, 2017 Aug.
[Is] ISSN:1537-2995
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: To bridge the gap between in vitro function and clinical efficacy of platelet (PLT) transfusion products, reliable in vivo PLT functional assays for hemostasis and survival in animal models are required. However, there are no standardized methods for assessing the in vivo quality of transfused human PLTs. STUDY DESIGN AND METHODS: Plasma-depleted human PLT concentrates (PCs; Day 3, Day 5, Day 7, Day 10, and damaged) were transfused into busulfan-induced rabbits with thrombocytopenia with prolonged bleeding times 1 day after treatment with ethyl palmitate (EP) to block their reticuloendothelial systems. The hemostatic effect of PC transfusion was evaluated by the ear fine vein bleeding time. For the in vivo survival assay, splenectomized EP-treated rabbits were transfused with human PCs, and viability of the human PLTs in the rabbits was determined by flow cytometry using human PLT-specific antibodies and Trucount tubes. RESULTS: The hemostatic effect of PCs was slightly reduced with increasing storage periods for early time points, but more dramatically reduced for later time points. PLT survival was similar after 3 and 7 days of storage, but PLTs stored for 10 days showed significantly poorer survival than those stored only 3 days. CONCLUSION: Our new and improved protocol for in vivo assessment of transfused PLTs is sufficiently sensitive to detect subtle changes in hemostatic function and viability of human PLTs transfused into rabbit models. This protocol could contribute to preclinical in vivo functional assessment and clinical quality assurance of emerging novel PLT products such as cultured cell-derived human PLTs.
[Mh] Termos MeSH primário: Plaquetas/citologia
Sobrevivência Celular
Hemostasia
Testes de Função Plaquetária/métodos
Transfusão de Plaquetas
[Mh] Termos MeSH secundário: Animais
Preservação de Sangue/métodos
Citometria de Fluxo/métodos
Seres Humanos
Métodos
Modelos Animais
Coelhos
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170707
[St] Status:MEDLINE
[do] DOI:10.1111/trf.14189


  9 / 231404 MEDLINE  
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[PMID]:28376393
[Au] Autor:Woods-Chabane GC; Glover CM; Marti EJ; Dickenson ERV
[Ad] Endereço:Southern Nevada Water Authority, P.O. Box 99954, Las Vegas, NV, 89193-9954, USA. Electronic address: gwen.woods-chabane@hdrinc.com.
[Ti] Título:A novel assay to measure tertiary and quaternary amines in wastewater: An indicator for NDMA wastewater precursors.
[So] Source:Chemosphere;179:298-305, 2017 Jul.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:This study examined the potential of using a novel bulk amine assay as an approximation for the tertiary and quaternary amine load in wastewaters and surface water samples, and this approximation was compared to N-nitrosodimethylamine (NDMA) formation potential using chloramines. An existing colorimetric method was examined and optimized for the detection of amines in environmental water samples. The method consists of liquid-liquid extraction followed by a catalyzed reaction to form a yet-undefined product that is known to be both a strong chromophore and fluorophore. Previous work verified that this reaction was effectively catalyzed by a number of compounds containing tertiary and quaternary amine moieties. Many tertiary and quaternary compounds are also efficient producers of NDMA under chloramination conditions, and a linear correlation was consequently derived from the bulk amine signals vs. NDMA formation potential in various wastewater samples (R = 0.74; n = 24; p-value < 0.05). The results provide evidence that approximately 2% of the tertiary and quaternary amines measured can form NDMA and an estimated 0.01-1.3% of nitrogen in dissolved organic nitrogen originates from these bulk amines. The normalization of NDMA concentration by the amine measurement revealed that ozone effectively destroyed those tertiary and quaternary amine structures more likely to form NDMA in treated wastewater samples. This bulk amine assay illustrates that proxy measurements of tertiary and quaternary amines can be linked to the NDMA formation potential of a given sample, and this approach may prove useful as a characterizing tool for NDMA precursors in wastewater.
[Mh] Termos MeSH primário: Aminas/análise
Dimetilnitrosamina/química
Águas Residuais/química
Purificação da Água/métodos
[Mh] Termos MeSH secundário: Aminas/química
Catálise
Cloraminas/química
Extração Líquido-Líquido
Métodos
Ozônio/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Chloramines); 0 (Waste Water); 66H7ZZK23N (Ozone); M43H21IO8R (Dimethylnitrosamine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170620
[Lr] Data última revisão:
170620
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170405
[St] Status:MEDLINE


  10 / 231404 MEDLINE  
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[PMID]:28350997
[Au] Autor:Jin C; Zhang Q; Lu W
[Ad] Endereço:School of Chemistry and Molecular Engineering, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China.
[Ti] Título:Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
[So] Source:Eur J Med Chem;132:135-141, 2017 May 26.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:We designed new hypoxia-activated prodrugs by conjugating (1-methyl-2-nitro-1H-imidazol-5-yl)methanol with 7-ethyl-10-hydroxy camptothecin (SN-38). Initially, we improved the method of multi-gram scale synthesis of (1-methyl-2-nitro-1H-imidazol-5-yl)methanol, which increased the yield to 42% compared to 8% by the original synthesis method. The improved method was used to synthesize evofosfamide (TH-302) and hypoxia-activated prodrugs of SN-38. Two different linkages between (1-methyl-2-nitro-1H-imidazol-5-yl)methanol and SN-38 were evaluated that afforded different hypoxia-selectivity and toxicity. Compound 16 (IOS), containing an ether linkage, was considered to be a promising hypoxia-selective antitumor agent.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Camptotecina/análogos & derivados
Hipóxia
Pró-Fármacos/síntese química
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/farmacocinética
Antineoplásicos/farmacologia
Camptotecina/química
Camptotecina/farmacocinética
Linhagem Celular Tumoral
Desenho de Drogas
Éter
Seres Humanos
Métodos
Camundongos
Microssomos Hepáticos/efeitos dos fármacos
Pró-Fármacos/farmacocinética
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Prodrugs); 0F5N573A2Y (Ether); 7673326042 (irinotecan); XT3Z54Z28A (Camptothecin)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170329
[St] Status:MEDLINE



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