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  1 / 20074 MEDLINE  
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[PMID]:29320822
[Au] Autor:Park GM; Park H; Oh S; Lee S
[Ad] Endereço:Department of Medical Environmental Biology, Catholic Kwandong University College of Medicine, Gangneung 25601, Korea.
[Ti] Título:Antimalarial Activity of C-10 Substituted Triazolyl Artemisinin.
[So] Source:Korean J Parasitol;55(6):661-665, 2017 Dec.
[Is] ISSN:1738-0006
[Cp] País de publicação:Korea (South)
[La] Idioma:eng
[Ab] Resumo:We synthesized C-10 substituted triazolyl artemisinins by the Huisgen cycloaddition reaction between dihydroartemisinins (2) and variously substituted 1, 2, 3-triazoles (8a-8h). The antimalarial activities of 32 novel artemisinin derivatives were screened against a chloroquine-resistant parasite. Among them, triazolyl artemisinins with electron-withdrawing groups showed stronger antimalarial activities than those shown by the derivatives having electron-donating groups. In particularly, m-chlorotriazolyl artemisinin (9d-12d) showed antimalarial activity equivalent to that of artemisinin and could be a strong drug candidate.
[Mh] Termos MeSH primário: Antimaláricos
Artemisininas/química
Triazóis/química
[Mh] Termos MeSH secundário: Reação de Cicloadição
Plasmodium falciparum/efeitos dos fármacos
Estereoisomerismo
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antimalarials); 0 (Artemisinins); 0 (Triazoles); 6A9O50735X (dihydroartemisinin)
[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:180112
[St] Status:MEDLINE
[do] DOI:10.3347/kjp.2017.55.6.661


  2 / 20074 MEDLINE  
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[PMID]:29274492
[Au] Autor:Çavusoglu BK; Yurttas L; Cantürk Z
[Ad] Endereço:Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir, Turkey. Electronic address: betulkaya@anadolu.edu.tr.
[Ti] Título:The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species.
[So] Source:Eur J Med Chem;144:255-261, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:In search of potent and safe antifungal agents, herein, we report the synthesis, characterization and biological activities of triazole-oxadiazole compounds. The structural verification of the molecules was carried out by H NMR, C NMR and mass spectral data. The in vitro antifungal and apoptotic activity were investigated against C. albicans, C. parapsilosis, C. krusei and C. glabrata. The compounds namely N-(4-nitrophenyl)-2-[(5-(2-((4-methyl-4H-1,2,4-triazol-3-yl)thio)ethyl)-1,3,4-oxadiazol-2-yl)thio]acetamide (4e) and N-(6-fluorobenzothiazol-2-yl)-2-[(5-(2-((4-methyl-4H-1,2,4-triazol-3-yl)thio)ethyl)-1,3,4-oxadiazol-2-yl)thio]acetamide (4i) were detected as the most potent compounds against C. albicans and C. glabrata (MIC = 62.5 µg/mL). According to studies on their mechanism of action, it was confirmed that compound 4i has apoptotic effect on four Candida via Annexin V-PI with flow cytometry. The MTT assay revealed that all compounds were determined to be non-toxic against healthy cells in the tested concentrations.
[Mh] Termos MeSH primário: Antifúngicos/química
Antifúngicos/farmacologia
Candida/efeitos dos fármacos
Oxidiazóis/química
Oxidiazóis/farmacologia
Triazóis/química
Triazóis/farmacologia
[Mh] Termos MeSH secundário: Antifúngicos/síntese química
Candidíase/tratamento farmacológico
Seres Humanos
Testes de Sensibilidade Microbiana
Oxidiazóis/síntese química
Relação Estrutura-Atividade
Triazóis/síntese química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antifungal Agents); 0 (Oxadiazoles); 0 (Triazoles)
[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:171224
[St] Status:MEDLINE


  3 / 20074 MEDLINE  
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[PMID]:29272750
[Au] Autor:Galibert M; Wartenberg M; Lecaille F; Saidi A; Mavel S; Joulin-Giet A; Korkmaz B; Brömme D; Aucagne V; Delmas AF; Lalmanach G
[Ad] Endereço:CNRS UPR 4301, Centre de Biophysique Moléculaire, Rue Charles Sadron, Orléans, France.
[Ti] Título:Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.
[So] Source:Eur J Med Chem;144:201-210, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Cathepsin (Cat) K is a critical bone-resorbing protease and is a relevant target for the treatment of osteoporosis and bone metastasis, while CatS is an attractive target for drugs in autoimmune diseases (e.g. rheumatoid arthritis), emphysema or neuropathic pain. Despite major achievements, current pharmacological inhibitors are still lacking in safety and may have damaging side effects. A promising strategy for developing safer reversible and competitive inhibitors as new lead compounds could be to insert non-cleavable bonds at the scissile P1-P1' position of selective substrates of CatS and CatK. Accordingly, we introduced a 1,4-disubstituted 1,2,3-triazole heterocycle that mimics most of the features of a trans-amide bond, or we incorporated a semicarbazide bond (azaGly residue) by replacing the α-carbon of the glycyl residue at P1 by a nitrogen atom. AzaGly-containing peptidomimetics inhibited powerfully their respective target proteases in the nM range, while triazolopeptides were weaker inhibitors (Ki in the µM range). The selectivity of the azaGly CatS inhibitor (1b) was confirmed by using spleen lysates from wild-type vs CatS-deficient mice. Alternatively, the azaGly bradykinin-derived CatK inhibitor (2b) potently inhibited CatK (Ki = 9 nM) and impaired its kininase activity in vitro. Molecular modeling studies support that the semicarbazide bond of 2b is more favorable than the 1,2,3-triazole linkage of the bradykinin-derived pseudopeptide 2a to preserve an effective affinity towards CatK, its protease target.
[Mh] Termos MeSH primário: Catepsina K/antagonistas & inibidores
Catepsinas/antagonistas & inibidores
Inibidores de Proteases/química
Inibidores de Proteases/farmacologia
Triazóis/química
Triazóis/farmacologia
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Animais
Catepsina K/metabolismo
Catepsinas/metabolismo
Seres Humanos
Camundongos Endogâmicos C57BL
Simulação de Acoplamento Molecular
Peptídeos/química
Peptídeos/farmacologia
Peptidomiméticos/química
Peptidomiméticos/farmacologia
Relação Estrutura-Atividade
Especificidade por Substrato
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Peptides); 0 (Peptidomimetics); 0 (Protease Inhibitors); 0 (Triazoles); EC 3.4.- (Cathepsins); EC 3.4.22.27 (cathepsin S); EC 3.4.22.38 (Cathepsin K)
[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:171223
[St] Status:MEDLINE


  4 / 20074 MEDLINE  
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[PMID]:28826030
[Au] Autor:Ahmed F; Perveen S; Shah K; Shah MR; Ahmed S
[Ad] Endereço:a International Center for Chemical and Biological Sciences, H.E.J. Research Institute of Chemistry, University of Karachi, Karachi 75270, Pakistan; Department of Chemistry, Women University of Azad Jammu & Kashmir Bagh, 12500, Pakistan. Electronic address: farids_ahmed@yahoo.com.
[Ti] Título:Synthesis and characterization of triazole based supramolecule for interaction with cefuroxime in tap water and blood plasma.
[So] Source:Ecotoxicol Environ Saf;147:49-54, 2018 Jan.
[Is] ISSN:1090-2414
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In this study a new calix[4]arene triazole 5 was successfully synthesized using click reaction and characterized through UV-visible, FT-IR, H NMR spectroscopes and Mass Spectrometry. The supramolecular interaction of compound 5 towards commonly used drugs has been carried out using UV-Visible spectroscopy. The supramolecule 5 showed characteristic enhancement in the absorbance intensity after mixing with Cefuroxime at pH (2-12). Compound 5 displayed considerably good interactions with cefuroxime in the presence of other drugs. Compound 5 exhibits linear relationship with cefuroxime concentration in the range of (10-80µM) with regression value of 0.9954. The standard deviation for 50µM Cefuroxime was found to be 0.01 and the limit of detection for cefuroxime was calculated to be 2µM. Job's plot experiments showed 1:1 (5: cefuroxime) binding stoichiometry between compound 5 and cefuroxime. Supramolecule 5 displayed fairly good spectrophotometric recognition of Cefuroxime in human blood plasma and tap water thus showing that the ingredients of tap water and plasma sample was inert in the recognition of cefuroxime.
[Mh] Termos MeSH primário: Calixarenos/química
Cefuroxima/sangue
Água Potável/química
Fenóis/química
Triazóis/síntese química
Poluentes Químicos da Água/sangue
[Mh] Termos MeSH secundário: Cefuroxima/análise
Seres Humanos
Técnicas In Vitro
Limite de Detecção
Espectroscopia de Ressonância Magnética
Plasma/química
Espectroscopia de Infravermelho com Transformada de Fourier
Triazóis/química
Poluentes Químicos da Água/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drinking Water); 0 (Phenols); 0 (Triazoles); 0 (Water Pollutants, Chemical); 0 (calix(4)arene); 130036-26-9 (Calixarenes); O1R9FJ93ED (Cefuroxime)
[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:170822
[St] Status:MEDLINE


  5 / 20074 MEDLINE  
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[PMID]:28922787
[Au] Autor:Blok EJ; Kroep JR; Meershoek-Klein Kranenbarg E; Duijm-de Carpentier M; Putter H; van den Bosch J; Maartense E; van Leeuwen-Stok AE; Liefers GJ; Nortier JWR; Rutgers EJT; van de Velde CJH; IDEAL Study Group
[Ad] Endereço:Departments of Surgery, Medical Oncology, and Medical Statistics, Leiden University Medical Center, Leiden, Netherlands; Department of Internal Medicine, Albert Schweitzer Hospital, Dordrecht, the Netherlands; Department of Internal Medicine, Reinier de Graaff Hospital, Delft, the Netherlands; Dutch
[Ti] Título:Optimal Duration of Extended Adjuvant Endocrine Therapy for Early Breast Cancer; Results of the IDEAL Trial (BOOG 2006-05).
[So] Source:J Natl Cancer Inst;110(1), 2018 Jan 01.
[Is] ISSN:1460-2105
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Background: The optimal duration of extended endocrine therapy beyond five years after initial aromatase inhibitor-based adjuvant therapy for postmenopausal women with hormone receptor-positive breast cancer is still unknown. Therefore, we conducted a clinical trial to compare two different extended endocrine therapy durations. Methods: In the randomized phase III IDEAL trial, postmenopausal patients with hormone receptor-positive breast cancer were randomly allocated to either 2.5 or five years of letrozole after the initial five years of any endocrine therapy. The primary end point was disease free survival (DFS), and secondary end points were overall survival (OS), distant metastasis-free interval (DMFi), new primary breast cancer, and safety. Hazard ratios (HRs) were determined using Cox regression analysis. All analyses were by intention-to-treat principle. Results: A total of 1824 patients were assigned to either 2.5 years (n = 909) or five years (n = 915) of letrozole, with a median follow-up of 6.6 years. A DFS event occurred in 152 patients in the five-year group, compared with 163 patients in the 2.5-year group (HR = 0.92, 95% confidence interval [CI] = 0.74 to 1.16). OS (HR = 1.04, 95% CI = 0.78 to 1.38) and DMFi (HR = 1.06, 95% CI = 0.78 to 1.45) were not different between both groups. A reduction in occurrence of second primary breast cancer was observed with five years of treatment (HR = 0.39, 95% CI = 0.19 to 0.81). Subgroup analysis did not identify patients who benefit from five-year extended therapy. Conclusion: This study showed no superiority of five years over 2.5 years of extended adjuvant letrozole after an initial five years of adjuvant endocrine therapy.
[Mh] Termos MeSH primário: Protocolos de Quimioterapia Combinada Antineoplásica/administração & dosagem
Neoplasias da Mama/terapia
Carcinoma Ductal de Mama/terapia
Carcinoma Intraductal não Infiltrante/terapia
Recidiva Local de Neoplasia/prevenção & controle
Segunda Neoplasia Primária/prevenção & controle
Nitrilos/administração & dosagem
Triazóis/administração & dosagem
[Mh] Termos MeSH secundário: Idoso
Protocolos de Quimioterapia Combinada Antineoplásica/efeitos adversos
Inibidores da Aromatase/administração & dosagem
Neoplasias da Mama/química
Neoplasias da Mama/patologia
Carcinoma Ductal de Mama/química
Carcinoma Ductal de Mama/prevenção & controle
Carcinoma Ductal de Mama/secundário
Carcinoma Intraductal não Infiltrante/prevenção & controle
Quimioterapia Adjuvante/efeitos adversos
Intervalo Livre de Doença
Feminino
Seguimentos
Seres Humanos
Mastectomia Segmentar
Meia-Idade
Nitrilos/efeitos adversos
Pós-Menopausa
Receptores Estrogênicos/análise
Receptores de Progesterona/análise
Taxa de Sobrevida
Tamoxifeno/administração & dosagem
Fatores de Tempo
Triazóis/efeitos adversos
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE III; COMPARATIVE STUDY; JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Aromatase Inhibitors); 0 (Nitriles); 0 (Receptors, Estrogen); 0 (Receptors, Progesterone); 0 (Triazoles); 094ZI81Y45 (Tamoxifen); 7LKK855W8I (letrozole)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170920
[St] Status:MEDLINE
[do] DOI:10.1093/jnci/djx134


  6 / 20074 MEDLINE  
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[PMID]:28859291
[Au] Autor:Heindl A; Sestak I; Naidoo K; Cuzick J; Dowsett M; Yuan Y
[Ad] Endereço:Centre for Evolution and Cancer, The Institute of Cancer Research, London, UK; Centre for Molecular Pathology, Royal Marsden Hospital, London, UK; Division of Molecular Pathology, The Institute of Cancer Research, London, UK; Centre for Cancer Prevention, Wolfson Institute of Preventive Medicine, Qu
[Ti] Título:Relevance of Spatial Heterogeneity of Immune Infiltration for Predicting Risk of Recurrence After Endocrine Therapy of ER+ Breast Cancer.
[So] Source:J Natl Cancer Inst;110(2), 2018 Feb 01.
[Is] ISSN:1460-2105
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Background: Despite increasing evidence supporting the clinical utility of immune infiltration in the estrogen receptor-negative (ER-) subtype, the prognostic value of immune infiltration for ER+ disease is not well defined. Methods: Quantitative immune scores of cell abundance and spatial heterogeneity were computed using a fully automated hematoxylin and eosin-stained image analysis algorithm and spatial statistics for 1178 postmenopausal patients with ER+ breast cancer treated with five years' tamoxifen or anastrozole. The prognostic significance of immune scores was compared with Oncotype DX 21-gene recurrence score (RS), PAM50 risk of recurrence (ROR) score, IHC4, and clinical treatment score, available for 963 patients. Statistical tests were two-sided. Results: Scores of immune cell abundance were not associated with recurrence-free survival. In contrast, high immune spatial scores indicating increased cell spatial clustering were associated with poor 10-year, early (0-5 years), and late (5-10 years) recurrence-free survival (Immune Hotspot: LR-χ2 = 14.06, P < .001, for 0-10 years; LR-χ2 = 6.24, P = .01, for 0-5 years; LR-χ2 = 7.89, P = .005, for 5-10 years). The prognostic value of spatial scores for late recurrence was similar to that of IHC4 and RS in both populations, but was not as strong as other tests in comparison for recurrence across 10 years. Conclusions: These results provide a missing link between tumor immunity and disease outcome in ER+ disease by examining tumor spatial architecture. The association between spatial scores and late recurrence suggests a lasting memory of protumor immunity that may impact disease progression and evolution of endocrine treatment resistance, which may be exploited for therapeutic advances.
[Mh] Termos MeSH primário: Neoplasias da Mama/imunologia
Neoplasias da Mama/patologia
Linfócitos do Interstício Tumoral/imunologia
Recidiva Local de Neoplasia/imunologia
Receptores Estrogênicos/análise
[Mh] Termos MeSH secundário: Idoso
Antineoplásicos/uso terapêutico
Biomarcadores Tumorais/imunologia
Neoplasias da Mama/química
Neoplasias da Mama/tratamento farmacológico
Intervalo Livre de Doença
Feminino
Seres Humanos
Contagem de Linfócitos
Meia-Idade
Nitrilos/uso terapêutico
Fatores de Risco
Tamoxifeno/uso terapêutico
Triazóis/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Biomarkers, Tumor); 0 (Nitriles); 0 (Receptors, Estrogen); 0 (Triazoles); 094ZI81Y45 (Tamoxifen); 2Z07MYW1AZ (anastrozole)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170902
[St] Status:MEDLINE
[do] DOI:10.1093/jnci/djx137


  7 / 20074 MEDLINE  
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[PMID]:29318321
[Au] Autor:Ziaie M; Dilmaghani KA; Tukmechi A
[Ti] Título:Synthesis and Biological Evaluation of 1,2,4-Triazoles and 1,3,4-Oxadiazoles Derivatives Linked to 1,4-Dihydropyridines Scaffold.
[So] Source:Acta Chim Slov;64(4):895-901, 2017 Dec.
[Is] ISSN:1318-0207
[Cp] País de publicação:Slovenia
[La] Idioma:eng
[Ab] Resumo:A series of diethyl-2,6-dimethyl-4-phenyl-1,4-dihydropyridine-3,5-dicarboxylate derivative coupled to 1,3,4-oxadiazole-5-thiones and 1,2,4-triazole-5-thiones moieties at C2,C6 positions of 1,4-dihydropyridine ring system was prepared. This linkage was carried out by the reaction of 1,3,4-oxadiazole-5-thiones and 1,2,4-triazole-5-thiones with 2,6-dibromomethyl-3,5-diethoxycarbonyl-4-phenyl-1,4-dihydropyridine in the presence of potassium carbonate as a weak base and dry acetone as the solvent. The newly synthesized compounds were characterized by FT-IR, 1H NMR, 13C NMR spectral data, elemental analysis and FAB-MS. The synthesized compounds were tested for their antimicrobial and antifungal activity against Escherichia coli and Aspergillus fumigatus in vitro in comparison with Enrofloxacin and Amphotericin as the reference drugs which are normally used for treating such infections. The synthetic compounds showed different inhibition zones against tested bacteria and fungi. Compound 8d showed more antagonistic activity against E. coli and A. fumigatus.
[Mh] Termos MeSH primário: Anti-Infecciosos/síntese química
Di-Hidropiridinas/química
Oxidiazóis/química
Triazóis/química
[Mh] Termos MeSH secundário: Anti-Infecciosos/farmacologia
Di-Hidropiridinas/farmacologia
Espectroscopia de Ressonância Magnética
Testes de Sensibilidade Microbiana
Oxidiazóis/farmacologia
Espectroscopia de Infravermelho com Transformada de Fourier
Triazóis/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Dihydropyridines); 0 (Oxadiazoles); 0 (Triazoles)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180306
[Lr] Data última revisão:
180306
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180111
[St] Status:MEDLINE


  8 / 20074 MEDLINE  
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[PMID]:29237530
[Au] Autor:Zhu XH; Li QG; Wang J; Hu GZ; Liu ZQ; Hu QH; Wu G
[Ad] Endereço:School of Medicine, Nanchang University, Nanchang 330006, China. nclqg2017@163.com.
[Ti] Título:[Mechanism of action of BET bromodomain inhibitor JQ1 in treating airway remodeling in asthmatic mice].
[So] Source:Zhongguo Dang Dai Er Ke Za Zhi;19(12):1278-1284, 2017 Dec.
[Is] ISSN:1008-8830
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:OBJECTIVE: To investigate the molecular mechanism of action of BET bromodomain inhibitor JQ1 in treating airway remodeling in asthmatic mice. METHODS: A total of 24 mice were randomly divided into control group, ovalbumin (OVA)-induced asthma group (OVA group), and JQ1 intervention group (JQ1+OVA group), with 8 mice in each group. OVA sensitization/challenge was performed to establish a mouse model of asthma. At 1 hour before challenge, the mice in the JQ1+OVA group were given intraperitoneal injection of JQ1 solution (50 µg/g). Bronchoalveolar lavage fluid (BALF) and lung tissue samples were collected at 24 hours after the last challenge, and the total number of cells and percentage of eosinophils in BALF were calculated. Pathological staining was performed to observe histopathological changes in lung tissue. RT-PCR and Western blot were used to measure the mRNA and protein expression of E-cadherin and vimentin during epithelial-mesenchymal transition (EMT). RESULTS: Compared with the control group, the OVA group had marked infiltration of inflammatory cells in the airway, thickening of the airway wall, increased secretion of mucus, and increases in the total number of cells and percentage of eosinophils in BALF (P<0.01). Compared with the OVA group, the JQ1+OVA group had significantly alleviated airway inflammatory response and significant reductions in the total number of cells and percentage of eosinophils in BALF (P<0.01). Compared with the control group, the OVA group had significant reductions in the mRNA and protein expression of E-cadherin and significant increases in the mRNA and protein expression of vimentin (P<0.01); compared with the OVA group, the JQ1+OVA group had significant increases in the mRNA and protein expression of E-cadherin and significant reductions in the mRNA and protein expression of vimentin (P<0.01); there were no significant differences in these indices between the JQ1+OVA group and the control group (P>0.05). CONCLUSIONS: Mice with OVA-induced asthma have airway remodeling during EMT. BET bromodomain inhibitor JQ1 can reduce airway inflammation, inhibit EMT, and alleviate airway remodeling, which provides a new direction for the treatment of asthma.
[Mh] Termos MeSH primário: Remodelação das Vias Aéreas/efeitos dos fármacos
Asma/tratamento farmacológico
Azepinas/farmacologia
Triazóis/farmacologia
[Mh] Termos MeSH secundário: Animais
Caderinas/análise
Caderinas/genética
Transição Epitelial-Mesenquimal
Feminino
Camundongos
Proteínas Nucleares/antagonistas & inibidores
Ovalbumina/imunologia
RNA Mensageiro/análise
Fatores de Transcrição/antagonistas & inibidores
Vimentina/análise
Vimentina/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 ((+)-JQ1 compound); 0 (Azepines); 0 (Brd4 protein, mouse); 0 (Cadherins); 0 (E-cadherin protein, mouse); 0 (Nuclear Proteins); 0 (RNA, Messenger); 0 (Transcription Factors); 0 (Triazoles); 0 (Vimentin); 9006-59-1 (Ovalbumin)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180306
[Lr] Data última revisão:
180306
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171215
[St] Status:MEDLINE


  9 / 20074 MEDLINE  
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[PMID]:29366931
[Au] Autor:Yadav N; Agarwal D; Kumar S; Dixit AK; Gupta RD; Awasthi SK
[Ad] Endereço:Chemical Biology Laboratory, Department of Chemistry, University of Delhi, Delhi, 110007, India.
[Ti] Título:In vitro antiplasmodial efficacy of synthetic coumarin-triazole analogs.
[So] Source:Eur J Med Chem;145:735-745, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Twenty two diverse coumarin-triazole derivatives were synthesized by alkylation of 7-hydroxy-4-methyl-coumarin followed by click chemistry at 7-position. These compounds were evaluated for their in vitro antiplasmodial activity against chloroquine sensitive strain of Plasmodium falciparum (3D7). Compound 9 (7-[1-(2, 4-dimethoxy-phenyl)-1H- [1-3] triazol-4-ylmethoxy]-4-methyl-chromen-2-one) was found most active with IC value 0.763 ±â€¯0.0124 µg/mL. Further, the structure of compound 20 was characterized by single crystal X-ray diffraction. In view of impressive results, we considered it worthwhile to validate the results of in vitro antiplasmodial activity by assessing whether these compounds are capable of hampering the catalytic activity of DNA gyrase, thus preventing its supercoiling function.
[Mh] Termos MeSH primário: Antimaláricos/farmacologia
Cumarínicos/farmacologia
Plasmodium falciparum/efeitos dos fármacos
Triazóis/farmacologia
[Mh] Termos MeSH secundário: Antimaláricos/síntese química
Antimaláricos/química
Linhagem Celular Tumoral
Sobrevivência Celular
Cumarínicos/química
DNA Girase/metabolismo
Relação Dose-Resposta a Droga
Escherichia coli/enzimologia
Seres Humanos
Estrutura Molecular
Testes de Sensibilidade Parasitária
Relação Estrutura-Atividade
Inibidores da Topoisomerase II/síntese química
Inibidores da Topoisomerase II/química
Inibidores da Topoisomerase II/farmacologia
Triazóis/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antimalarials); 0 (Coumarins); 0 (Topoisomerase II Inhibitors); 0 (Triazoles); A4VZ22K1WT (coumarin); EC 5.99.1.3 (DNA Gyrase)
[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:180126
[St] Status:MEDLINE


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[PMID]:29289884
[Au] Autor:Reddy VG; Bonam SR; Reddy TS; Akunuri R; Naidu VGM; Nayak VL; Bhargava SK; Kumar HMS; Srihari P; Kamal A
[Ad] Endereço:Academy of Scientific and Innovative Research (AcSIR), CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad, 500007, India; Medicinal Chemistry and Biotechnology, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad, 500007, India; Division of Natural Products Chemistry, CSIR-Ind
[Ti] Título:4ß-amidotriazole linked podophyllotoxin congeners: DNA topoisomerase-IIα inhibition and potential anticancer agents for prostate cancer.
[So] Source:Eur J Med Chem;144:595-611, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Topoisomerases (topo-I and topo-II) have occupied a significant role in DNA replication, transcription, and are a promising set of antitumor targets. In the present approach, a series of new 4ß-amidotriazole linked podophyllotoxin derivatives (10a-i and 11a-k) were designed, synthesized by employing the click chemistry and their biological activities were evaluated. The majority of derivatives showed promising antiproliferative activity with IC values ranging from 1 to 10 µM on the six human cancer cell lines; cervical (HeLa), breast (MCF-7), prostate (DU-145), lung (A549), liver (HepG2) and colon (HT-29). Among them, some of the congeners 10b, 10g and 10i have shown remarkable cytotoxicity with IC values of, < 1 µM against the tested cancer cell lines and found to be more active than etoposide. Topoisomerase-mediated DNA relaxation assay results showed that the derivatives could efficiently inhibit the activity of topoisomerase-II. In addition, flow cytometry analysis on DU-145 cells revealed that these compounds arrest G2/M phase of cell cycle. Further apoptotic studies were also performed on these DU-145 cells, which showed that this class of compounds could induce apoptosis effectively.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
DNA Topoisomerases Tipo II/metabolismo
Podofilotoxina/farmacologia
Neoplasias da Próstata/tratamento farmacológico
Inibidores da Topoisomerase II/farmacologia
Triazóis/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Apoptose/efeitos dos fármacos
Ciclo Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Seres Humanos
Masculino
Potencial da Membrana Mitocondrial/efeitos dos fármacos
Simulação de Acoplamento Molecular
Estrutura Molecular
Podofilotoxina/química
Neoplasias da Próstata/metabolismo
Neoplasias da Próstata/patologia
Espécies Reativas de Oxigênio/análise
Espécies Reativas de Oxigênio/metabolismo
Relação Estrutura-Atividade
Inibidores da Topoisomerase II/síntese química
Inibidores da Topoisomerase II/química
Triazóis/síntese química
Triazóis/química
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Reactive Oxygen Species); 0 (Topoisomerase II Inhibitors); 0 (Triazoles); EC 5.99.1.3 (DNA Topoisomerases, Type II); L36H50F353 (Podophyllotoxin)
[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:180101
[St] Status:MEDLINE



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