Base de dados : MEDLINE
Pesquisa : D02.145 [Categoria DeCS]
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[PMID]:29291442
[Au] Autor:Zong G; Sun X; Bhakta R; Whisenhunt L; Hu Z; Wang F; Shi WQ
[Ad] Endereço:Department of Chemistry and Biochemistry, J. William Fulbright College of Arts & Science, University of Arkansas, Fayetteville, AR, 72701, USA.
[Ti] Título:New insights into structure-activity relationship of ipomoeassin F from its bioisosteric 5-oxa/aza analogues.
[So] Source:Eur J Med Chem;144:751-757, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Ipomoeassin F, a plant-derived macrolide, exhibited single-digit nanomolar growth inhibition activity against many cancer cell lines. In this report, a series of 5-oxa/aza analogues was prepared and screened for cytotoxicity. Replacement of 5-CH with O/NH simplified the synthesis and led to only a small activity loss. N-methylation almost completely restored the potency. Further studies with additional 5-oxa analogues suggested, for the first time, that size and flexibility of the ring also significantly influence the bioactivity of ipomoeassin F.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Compostos Aza/farmacologia
Glicoconjugados/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Compostos Aza/química
Linhagem Celular
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Glicoconjugados/síntese química
Glicoconjugados/química
Seres Humanos
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Aza Compounds); 0 (Glycoconjugates); 0 (ipomoeassin F)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180102
[St] Status:MEDLINE


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[PMID]:29220516
[Au] Autor:Depalo L; Lanzoni A; Masetti A; Pasqualini E; Burgio G
[Ad] Endereço:Dipartimento di Scienze Agrarie-Entomologia, Alma Mater Studiorum-Università di Bologna, Italy.
[Ti] Título:Lethal and Sub-lethal Effects of Four Insecticides on the Aphidophagous Coccinellid Adalia bipunctata (Coleoptera: Coccinellidae).
[So] Source:J Econ Entomol;110(6):2662-2671, 2017 12 05.
[Is] ISSN:1938-291X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Conventional insecticide assays, which measure the effects of insecticide exposure on short-term mortality, overlook important traits, including persistence of toxicity or sub-lethal effects. Therefore, such approaches are especially inadequate for prediction of the overall impact of insecticides on beneficial arthropods. In this study, the side effects of four modern insecticides (chlorantraniliprole, emamectin benzoate, spinosad, and spirotetramat) on Adalia bipunctata (L.) (Coleoptera: Coccinellidae) were evaluated under laboratory conditions by exposition on treated potted plants. In addition to investigation of acute toxicity and persistence of harmful activity in both larvae and adults of A. bipunctata, demographic parameters were evaluated, to provide a comprehensive picture of the nontarget effects of these products. Field doses of the four insecticides caused detrimental effects to A. bipunctata; but in different ways. Overall, spinosad showed the best toxicological profile among the products tested. Emamectin benzoate could be considered a low-risk insecticide, but had high persistence. Chlorantraniliprole exhibited lethal effects on early instar larvae and adults, along with a long-lasting activity, instead spirotetramat showed a low impact on larval and adult mortality and can be considered a short-lived insecticide. However, demographic analysis demonstrated that chlorantraniliprole and spirotetramat caused sub-lethal effects. Our findings highlight that sole assessment of mortality can lead to underestimation of the full impact of pesticides on nontarget insects. Demographic analysis was demonstrated to be a sensitive method for detection of the sub-lethal effects of insecticides on A. bipunctata, and this approach should be considered for evaluation of insecticide selectivity.
[Mh] Termos MeSH primário: Coleópteros/efeitos dos fármacos
Inseticidas/toxicidade
[Mh] Termos MeSH secundário: Animais
Compostos Aza/toxicidade
Coleópteros/crescimento & desenvolvimento
Combinação de Medicamentos
Ivermectina/análogos & derivados
Ivermectina/toxicidade
Larva/efeitos dos fármacos
Larva/crescimento & desenvolvimento
Macrolídeos/toxicidade
Compostos de Espiro/toxicidade
ortoaminobenzoatos/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Aza Compounds); 0 (Drug Combinations); 0 (Insecticides); 0 (Macrolides); 0 (Spiro Compounds); 0 (ortho-Aminobenzoates); 4G7KR034OX (spirotetramat); 622AK9DH9G (chlorantranilipole); 70288-86-7 (Ivermectin); HVM3G4A01W (emamectin benzoate); XPA88EAP6V (spinosad)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171209
[St] Status:MEDLINE
[do] DOI:10.1093/jee/tox243


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[PMID]:29319078
[Au] Autor:De Simone BC; Mazzone G; Russo N; Sicilia E; Toscano M
[Ad] Endereço:Dipartimento di Chimica e Tecnologie Chimiche, Università della Calabria, 87036 Rende (CS), Italy. desimone@unical.it gloria.mazzone@unical.it.
[Ti] Título:Excitation energies, singlet-triplet energy gaps, spin-orbit matrix elements and heavy atom effects in BOIMPYs as possible photosensitizers for photodynamic therapy: a computational investigation.
[So] Source:Phys Chem Chem Phys;20(4):2656-2661, 2018 Jan 24.
[Is] ISSN:1463-9084
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Bis(borondifluoride)-8-imidazodipyrromethene (BOIMPY) based molecules show interesting photophysical properties. We have undertaken a computational study at DFT and TDDFT levels of theory with the aim of verifying if the non-fluorescent BOIMPYs meet those properties necessary to be proposed as potential photosensitizers for photodynamic therapy (PDT). In particular, we have computed the absorption wavelengths, the singlet-triplet energy gaps and the spin-orbit matrix elements. The effect of halogen atom substitution (Br, I), in different amounts and positions in the BOIMPY skeleton, on the photophysical properties, has been elucidated. Some possible pathways for the population of the lowest triplet state have been examined and rationalized on the basis of Kasha rules. The results indicate that many of the studied systems can be indicated as potential photosensitizers for photodynamic therapy.
[Mh] Termos MeSH primário: Compostos Aza/química
Modelos Moleculares
Fármacos Fotossensibilizantes/química
[Mh] Termos MeSH secundário: Fotoquimioterapia
Teoria Quântica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Aza Compounds); 0 (Photosensitizing Agents)
[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:180111
[St] Status:MEDLINE
[do] DOI:10.1039/c7cp06763a


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[PMID]:28463435
[Au] Autor:Peng T; Chen X; Pan Y; Zheng Z; Wei X; Xi J; Zhang J; Gao X; Shang Q
[Ad] Endereço:College of Plant Science, Jilin University, Changchun, China.
[Ti] Título:Transcription factor aryl hydrocarbon receptor/aryl hydrocarbon receptor nuclear translocator is involved in regulation of the xenobiotic tolerance-related cytochrome P450 CYP6DA2 in Aphis gossypii Glover.
[So] Source:Insect Mol Biol;26(5):485-495, 2017 10.
[Is] ISSN:1365-2583
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The cotton aphid, Aphis gossypii, is one of the most economically important agricultural pests worldwide as it is polyphagous and resistant to many classes of insecticides. Overexpression of the cytochrome P450 monooxygenase (P450) CYP6DA2 has previously been found to be associated with gossypol and spirotetramat tolerance in the cotton aphid. In the present study, the elements located in the promoter region (-357:-343; -250:-241; -113:-104) of CYP6DA2 were shown to control promoter activity, and gossypol induction was observed. We hypothesized that the expression of CYP6DA2 is subject to transcriptional regulation. To investigate the underlying mechanism, we assessed two transcription factors, aryl hydrocarbon receptor (AhR) and aryl hydrocarbon receptor nuclear translocator (ARNT), and found that the abundance of AhR was highly correlated with CYP6DA2 abundance. RNA interference of AhR or ARNT significantly decreased the levels of the target gene as well as those of its counterpart, and both dramatically repressed CYP6DA2 expression. Cotransfection of the ARNT, AhR, or AhR plus ARNT and CYP6DA2 promoter constructs elevated CYP6DA2 promoter activity, with the AhR plus ARNT cotransfection being the most effective. Thus, these elements located in the promoter were responsible for CYP6DA2 transcription, and CYP6DA2 expression was regulated by the transcription factors AhR and ARNT.
[Mh] Termos MeSH primário: Afídeos/metabolismo
Translocador Nuclear Receptor Aril Hidrocarboneto/metabolismo
Família 6 do Citocromo P450/metabolismo
Receptores de Hidrocarboneto Arílico/metabolismo
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Animais
Afídeos/genética
Compostos Aza
Sequência de Bases
Sequência Conservada
Família 6 do Citocromo P450/genética
Técnicas de Silenciamento de Genes
Gossipol
Proteínas de Insetos/metabolismo
Resistência a Inseticidas
Dados de Sequência Molecular
Regiões Promotoras Genéticas
Compostos de Espiro
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Aza Compounds); 0 (Insect Proteins); 0 (Receptors, Aryl Hydrocarbon); 0 (Spiro Compounds); 138391-32-9 (Aryl Hydrocarbon Receptor Nuclear Translocator); 4G7KR034OX (spirotetramat); EC 1.14.14.1 (Cytochrome P450 Family 6); KAV15B369O (Gossypol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:180111
[Lr] Data última revisão:
180111
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE
[do] DOI:10.1111/imb.12311


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[PMID]:28946322
[Au] Autor:Faraji M; Noorbakhsh R; Shafieyan H; Ramezani M
[Ad] Endereço:Faculty of Food Industry and Agriculture, Department of Food science & Technology, Standard Research Institute (SRI), Karaj, P.O. Box 31745-139, Iran. Electronic address: mohammadfaraji2010@gmail.com.
[Ti] Título:Determination of acetamiprid, imidacloprid, and spirotetramat and their relevant metabolites in pistachio using modified QuEChERS combined with liquid chromatography-tandem mass spectrometry.
[So] Source:Food Chem;240:634-641, 2018 Feb 01.
[Is] ISSN:0308-8146
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A QuEChERS based methodology was developed for the simultaneous identification and quantification of acetamiprid, imidacloprid, and spirotetramat and their relevant metabolites in pistachio by liquid chromatography-tandem mass spectrometry for the first time. First, sample extraction was done with MeCN:citrate buffer:NaHCO followed by phase separation with the addition of MgSO :NaCl. The supernatant was then cleaned by a primary-secondary amine (PSA), GCB, and MgSO . The proposed method provides a linearity in the range of 5-200µgL , and the linear regression coefficients were higher than 0.99. LOD and LOQ were obtained to be 2 and 5µgkg for the studied insecticides, respectively, with the exception of imidacloprid-olefin (5 and 10µgkg ). Acceptable recoveries (91-110%) were obtained for all the analytes with good intra- and inter-precisions (0.4≥RSD ≤11.0). The method was then used for the pistachio samples collected from a field trial to estimate the maximum residue limits (MRLs) in next step.
[Mh] Termos MeSH primário: Pistacia
[Mh] Termos MeSH secundário: Compostos Aza
Cromatografia Líquida de Alta Pressão
Neonicotinoides
Nitrocompostos
Compostos de Espiro
Espectrometria de Massas em Tandem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Aza Compounds); 0 (Neonicotinoids); 0 (Nitro Compounds); 0 (Spiro Compounds); 3BN7M937V8 (imidacloprid); 4G7KR034OX (spirotetramat); 5HL5N372P0 (acetamiprid)
[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:170927
[St] Status:MEDLINE


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[PMID]:27776972
[Au] Autor:McCubrey JA; Lertpiriyapong K; Fitzgerald TL; Martelli AM; Cocco L; Rakus D; Gizak A; Libra M; Cervello M; Montalto G; Yang LV; Abrams SL; Steelman LS
[Ad] Endereço:Department of Microbiology & Immunology, Brody School of Medicine, East Carolina University, Greenville, NC 27834, USA. Electronic address: mccubreyj@ecu.edu.
[Ti] Título:Roles of TP53 in determining therapeutic sensitivity, growth, cellular senescence, invasion and metastasis.
[So] Source:Adv Biol Regul;63:32-48, 2017 Jan.
[Is] ISSN:2212-4934
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:TP53 is a critical tumor suppressor gene that regulates cell cycle progression, apoptosis, cellular senescence and many other properties critical for control of normal cellular growth and death. Due to the pleiotropic effects that TP53 has on gene expression and cellular physiology, mutations at this tumor suppressor gene result in diverse physiological effects. T53 mutations are frequently detected in numerous cancers. The expression of TP53 can be induced by various agents used to treat cancer patients such as chemotherapeutic drugs and ionizing radiation. Radiation will induce Ataxia telangiectasia mutated (ATM) and other kinases that results in the phosphorylation and activation of TP53. TP53 is also negatively regulated by other mechanisms, such as ubiquitination by ligases such as MDM2. While TP53 has been documented to control the expression of many "classical" genes (e.g., p21 , PUMA, Bax) by transcriptional mechanisms for quite some time, more recently TP53 has been shown to regulate microRNA (miR) gene expression. Different miRs can promote oncogenesis (oncomiR) whereas others act to inhibit tumor progression (tumor suppressor miRs). Targeted therapies to stabilize TP53 have been developed by various approaches, MDM2/MDM4 inhibitors have been developed to stabilize TP53 in TP53-wild type (WT) tumors. In addition, small molecules have been isolated that will reactivate certain mutant TP53s. Both of these types of inhibitors are in clinical trials. Understanding the actions of TP53 may yield novel approaches to suppress cancer, aging and other health problems.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Compostos Aza/farmacologia
Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia
Ciclo Celular/efeitos dos fármacos
Regulação Neoplásica da Expressão Gênica
Neoplasias/genética
Proteína Supressora de Tumor p53/agonistas
[Mh] Termos MeSH secundário: Proteínas Reguladoras de Apoptose/genética
Proteínas Reguladoras de Apoptose/metabolismo
Ciclo Celular/genética
Proliferação Celular/efeitos dos fármacos
Senescência Celular
Inibidor de Quinase Dependente de Ciclina p21/genética
Inibidor de Quinase Dependente de Ciclina p21/metabolismo
Seres Humanos
MicroRNAs/genética
MicroRNAs/metabolismo
Invasividade Neoplásica
Metástase Neoplásica
Neoplasias/tratamento farmacológico
Neoplasias/metabolismo
Neoplasias/patologia
Proteínas Proto-Oncogênicas/genética
Proteínas Proto-Oncogênicas/metabolismo
Transdução de Sinais
Proteína Supressora de Tumor p53/genética
Proteína Supressora de Tumor p53/metabolismo
Proteína X Associada a bcl-2/genética
Proteína X Associada a bcl-2/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (2,2-bis(hydroxymethyl)-1-azabicyclo(2,2,2,)octan-3-one); 0 (Antineoplastic Agents); 0 (Apoptosis Regulatory Proteins); 0 (Aza Compounds); 0 (BAX protein, human); 0 (BBC3 protein, human); 0 (Bridged Bicyclo Compounds, Heterocyclic); 0 (Cyclin-Dependent Kinase Inhibitor p21); 0 (MicroRNAs); 0 (Proto-Oncogene Proteins); 0 (Tumor Suppressor Protein p53); 0 (bcl-2-Associated X Protein)
[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:161026
[St] Status:MEDLINE


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[PMID]:28886889
[Au] Autor:Suslov E; Zarubaev VV; Slita AV; Ponomarev K; Korchagina D; Ayine-Tora DM; Reynisson J; Volcho K; Salakhutdinov N
[Ad] Endereço:Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia.
[Ti] Título:Anti-influenza activity of diazaadamantanes combined with monoterpene moieties.
[So] Source:Bioorg Med Chem Lett;27(19):4531-4535, 2017 10 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The antiviral activity of several diaza-adamantanes containing monoterpenoid moieties against a rimantadine-resistant strain of the influenza A/Puerto Rico/8/34 (H1N1) virus was studied. Hetero-adamantanes containing monoterpene moieties at the aminal position of the heterocycle were found to exhibit lower activity compared to compounds with a diaza-adamantane fragment and a monoterpene moiety linked via an amino group at the 6-position of the hetero-adamantane ring. The highest selectivity index (a ratio of the 50% cytotoxic concentration to the 50% inhibitory concentration) out of 30 was observed for compound 8d, which contains a citronellal monoterpenoid moiety. Diaza-adamantane 8d was superior to its adamantane-containing analog 5 both in its anti-influenza activity and selectivity. Furthermore, 8d has more balanced physicochemical properties than 5, making the former a more promising drug candidate. Modelling these compounds against an influenza virus M2 ion channel predicted plausible binding modes to both the wild-type and the mutant (S31N).
[Mh] Termos MeSH primário: Adamantano/farmacologia
Antivirais/farmacologia
Compostos Aza/farmacologia
Vírus da Influenza A Subtipo H1N1/efeitos dos fármacos
Monoterpenos/farmacologia
[Mh] Termos MeSH secundário: Adamantano/química
Antivirais/síntese química
Antivirais/química
Compostos Aza/química
Relação Dose-Resposta a Droga
Testes de Sensibilidade Microbiana
Estrutura Molecular
Monoterpenos/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (Aza Compounds); 0 (Monoterpenes); PJY633525U (Adamantane)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170910
[St] Status:MEDLINE


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[PMID]:28671827
[Au] Autor:Galasiti Kankanamalage AC; Kim Y; Rathnayake AD; Alliston KR; Butler MM; Cardinale SC; Bowlin TL; Groutas WC; Chang KO
[Ad] Endereço:Department of Chemistry, Wichita State University , Wichita, Kansas 67260, United States.
[Ti] Título:Design, Synthesis, and Evaluation of Novel Prodrugs of Transition State Inhibitors of Norovirus 3CL Protease.
[So] Source:J Med Chem;60(14):6239-6248, 2017 Jul 27.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Ester and carbamate prodrugs of aldehyde bisulfite adduct inhibitors were synthesized in order to improve their pharmacokinetic and pharmacodynamic properties. The inhibitory activity of the compounds against norovirus 3C-like protease in enzyme and cell-based assays was determined. The ester and carbamate prodrugs displayed equivalent potency to those of the precursor aldehyde bisulfite adducts and precursor aldehydes. Furthermore, the rate of ester cleavage was found to be dependent on alkyl chain length. The generated prodrugs exhibited low cytotoxicity and satisfactory liver microsomes stability and plasma protein binding. The methodology described herein has wide applicability and can be extended to the bisulfite adducts of common warheads employed in the design of transition state inhibitors of serine and cysteine proteases of medical relevance.
[Mh] Termos MeSH primário: Antivirais/química
Compostos Aza/química
Carbamatos/química
Cisteína Endopeptidases/metabolismo
Inibidores de Cisteína Proteinase/química
Norovirus/efeitos dos fármacos
Pró-Fármacos/química
Pirrolidinas/química
Proteínas Virais/antagonistas & inibidores
[Mh] Termos MeSH secundário: Animais
Antivirais/síntese química
Antivirais/farmacologia
Compostos Aza/síntese química
Compostos Aza/farmacologia
Proteínas Sanguíneas/metabolismo
Carbamatos/síntese química
Carbamatos/farmacologia
Linhagem Celular
Inibidores de Cisteína Proteinase/síntese química
Inibidores de Cisteína Proteinase/farmacologia
Ésteres/síntese química
Ésteres/química
Ésteres/farmacologia
Seres Humanos
Hidrólise
Camundongos
Microssomos Hepáticos/metabolismo
Modelos Moleculares
Pró-Fármacos/síntese química
Pró-Fármacos/farmacologia
Ligação Proteica
Pirrolidinas/síntese química
Pirrolidinas/farmacologia
Estereoisomerismo
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (Aza Compounds); 0 (Blood Proteins); 0 (Carbamates); 0 (Cysteine Proteinase Inhibitors); 0 (Esters); 0 (Prodrugs); 0 (Pyrrolidines); 0 (Viral Proteins); EC 3.4.22.- (Cysteine Endopeptidases)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170906
[Lr] Data última revisão:
170906
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170704
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.7b00497


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[PMID]:28628723
[Au] Autor:Vultos F; Fernandes C; Mendes F; Marques F; Correia JDG; Santos I; Gano L
[Ad] Endereço:Centro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, km 139.7, 2695-066, Bobadela, LRS, Portugal.
[Ti] Título:A Multifunctional Radiotheranostic Agent for Dual Targeting of Breast Cancer Cells.
[So] Source:ChemMedChem;12(14):1103-1107, 2017 Jul 20.
[Is] ISSN:1860-7187
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:A straightforward synthetic route for a new multifunctional 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) derivative is described. To demonstrate the versatility of this pro-chelator for the preparation of radiolabeled hybrid compounds containing two different biological targeting moieties, an antitumor agent (e.g., a DNA-intercalating agent) and an estrogen receptor (ER) ligand (e.g., LXXLL-based peptide) were regiospecifically conjugated to the DOTA derivative. The bifunctional probe was radiolabeled with the auger electron emitter indium-111, and the resulting radioconjugate was demonstrated to induce DNA damage in vitro, which, along with the nuclear internalization exhibited in breast cancer cells, might enhance its therapeutic activity. This favorable in vitro performance suggests that these hybrid compounds could be attractive probes for theranostic applications.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Compostos Aza/síntese química
Compostos Heterocíclicos com 1 Anel/síntese química
Compostos Radiofarmacêuticos/síntese química
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/farmacologia
Compostos Aza/farmacologia
Neoplasias da Mama
Sobrevivência Celular/efeitos dos fármacos
Quelantes/química
Feminino
Compostos Heterocíclicos com 1 Anel/farmacologia
Seres Humanos
Radioisótopos de Índio
Substâncias Intercalantes/química
Ligantes
Células MCF-7
Camundongos
Peptídeos/química
Ligação Proteica
Compostos Radiofarmacêuticos/farmacologia
Receptores Estrogênicos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetracetic acid); 0 (Antineoplastic Agents); 0 (Aza Compounds); 0 (Chelating Agents); 0 (Heterocyclic Compounds, 1-Ring); 0 (Indium Radioisotopes); 0 (Intercalating Agents); 0 (Ligands); 0 (Peptides); 0 (Radiopharmaceuticals); 0 (Receptors, Estrogen)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170620
[St] Status:MEDLINE
[do] DOI:10.1002/cmdc.201700287


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[PMID]:28558195
[Au] Autor:Rajarathinam B; Kumaravel K; Vasuki G
[Ad] Endereço:Department of Chemistry, Pondicherry University , Puducherry 605 014, India.
[Ti] Título:"In Water": Organocatalyzed Diastereoselective Multicomponent Reactions toward 2-Azapyrrolizidine Alkaloid Scaffolds.
[So] Source:ACS Comb Sci;19(7):455-463, 2017 Jul 10.
[Is] ISSN:2156-8944
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Synthesis of the 2-aza analogues of pyrrolizidine and spirooxindole-2-azapyrrolizidine hybrid, a spiro-tetracyclic scaffold possessing multiple contiguous stereocenters, by an exclusive regio-, chemo-, and diastereoselective multicomponent reaction in water is reported. This logical and didactical tactic has integrated the principles of an ideal organic synthesis, privileged substructure-based diversity-oriented synthesis, and biology-oriented synthesis to access hybrid heterocyclic scaffolds.
[Mh] Termos MeSH primário: Compostos Aza/síntese química
Alcaloides de Pirrolizidina/síntese química
Água/química
[Mh] Termos MeSH secundário: Catálise
Ciclização
Estrutura Molecular
Solubilidade
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Aza Compounds); 0 (Pyrrolizidine Alkaloids); 059QF0KO0R (Water)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170531
[St] Status:MEDLINE
[do] DOI:10.1021/acscombsci.7b00038



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