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  1 / 19721 MEDLINE  
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[PMID]:29314204
[Au] Autor:Jin Z; Tan Q; Sun B
[Ad] Endereço:State Key Laboratory of Biomembrane and Membrane Biotechnology, School of Medicine, Tsinghua University, Beijing, China.
[Ti] Título:Telmisartan ameliorates vascular endothelial dysfunction in coronary slow flow phenomenon (CSFP).
[So] Source:Cell Biochem Funct;36(1):18-26, 2018 Jan.
[Is] ISSN:1099-0844
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Coronary slow flow phenomenon (CSFP) is a coronary microvascular disorder with an increasing morbidity, and currently, available therapies are of limited clinical value for its cure. Hence, it is urgent to find a novel approach to CSFP treatment. Several studies show that endothelial dysfunction plays a critical role in the aetiology of CSFP. Telmisartan (TMST) is a clinically available anti-hypertensive medicine and has shown its potential properties for improving vascular endothelial function. Thus, we aimed to investigate the effect of TMST on endothelial dysfunction in CSFP, Endothelial-dependent flow-mediated vasodilation, serum levels of nitric oxide, adiponectin, and endothelin-1 were surveyed before and after 3 months of TMST treatment. And the percentages of vasodilator response to acetylcholine (Ach) were detected after 12 weeks of TMST treatment. Compare with pretreatment, flow-mediated vasodilation, nitric oxide, and adiponectin were substantially improved after TMST treatment; meanwhile, endothelin-1 was decreased in the TMST group (all P < .01). Compared with the model group, the vasodilator response to Ach was enormously increased after TMST intervention. Additionally, administration of SU11274 or GW9662 would partially reverse the protective effects of TMST on accumulative concentration-vasodilator responses to Ach (P < .01). We demonstrated that administration of TMST could remarkably increase the mRNA and/or protein levels of hepatocyte growth factor, mesenchymal-epithelial transition factor, peroxisome proliferation-activated receptor γ, whereas dramatically diminish mRNA and/or protein levels of p-JNK1/2, mitogen-activated protein kinase, and nuclear factor kappa B (P < .05). Our results thus implicate that TMST ameliorates endothelial dysfunction in CSFP. It is suggested that TSMF may play an important role in the medication of CSFP.
[Mh] Termos MeSH primário: Benzimidazóis/farmacologia
Benzimidazóis/uso terapêutico
Benzoatos/farmacologia
Benzoatos/uso terapêutico
Endotélio Vascular/efeitos dos fármacos
Endotélio Vascular/fisiopatologia
Fenômeno de não Refluxo/tratamento farmacológico
[Mh] Termos MeSH secundário: Angiotensina II/farmacologia
Animais
Benzimidazóis/química
Benzoatos/química
Relação Dose-Resposta a Droga
Endotélio Vascular/metabolismo
Feminino
Seres Humanos
Masculino
Meia-Idade
Coelhos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzimidazoles); 0 (Benzoates); 11128-99-7 (Angiotensin II); U5SYW473RQ (telmisartan)
[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:180110
[St] Status:MEDLINE
[do] DOI:10.1002/cbf.3313


  2 / 19721 MEDLINE  
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[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


  3 / 19721 MEDLINE  
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[PMID]:29203736
[Au] Autor:Lutsenko RV; Vlasova EV; Kolot EG; Gladka VM; Sidorenko AG
[Ad] Endereço:Higher State Educational Establishment Of Ukraine, "Ukrainian Medical Stomatological Academy", Poltava, Ukraine.
[Ti] Título:The exchange of monoamines during the experimental neurosis on the background of using of amide "2-hydroxy-n-naphthalen-1-yl-2-(2-oxo-,2-dihydroindol-3-ylidene)".
[So] Source:Wiad Lek;70(5):895-900, 2017.
[Is] ISSN:0043-5147
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Incessant increase in the frequency and distribution of anxiety disorders stipulates searching, research and study of the mechanism of action of new substances for their correction, including the group of 2-oxoindolin-3-glyoxylic acid derivatives. THE AIM: To research the effect of N-(1-naphthyl) amide-2-oxoindolin-3-glyoxylic acid on monoaminergic system of subjected to experimental neurosis of rats. MATERIALS AND METHODS: The experiments were performed on male Wistar rats, who have weight 180-220g and were researching the effect of 2-hydro-N-naphthalen-1-yl-2-(2-oxy-1,2-dihydroindol-3-ylidene)-acetamide (compound 18) at a dose (12 mg/kg), by intragastric drug injection of subjected to experimental neurosis rats, during 30 days (1 time in three days), for monoamines content (epinephrine, norepinephrine, dopamine and serotonin) in the blood, their decay products (homovanillic acid, vanillylmandelic acid and 5-oxyindolacetic acid) in the urine and the ratio of end products of the reaction to their predecessors. RESEARCH: It was established that during the preventive-therapeutic application of N-(1-naphthyl)amide-2-oxoindolin-3-glyoxylic acid, it effectively adjusts the level of monoamines, reducing the content of adrenaline and increasing the content of noradrenaline, dopamine and 5-HT in the blood. The compound also reduces the content of products exchange of mediators (HVA,VMA and 5-OIAA) in the urine. The 2-oxoindolin derivatives reduces the ratio between HVA/dopamine, VMA/(noradrenaline + adrenaline) and 5-OIAA/5-HT, it testifies about the normalizing of enzymes activity, which are involved in the process of exchange and maintaining the constancy of monoamines. The results show that in the mechanisms of anxiolytic action of compound 18, a significant role plays the normalization of content and exchange of neurotransmitters in the organism, which caused an experimental neurosis. CONCLUSION: Compound 2-hydro-N-naphthalen-1-yl-2-(2-oxo-1,2-dihydroindol-3-ylidene)-acetamide by the experimental 30-day neurosis, was reducing the expression of neurotransmitter imbalance in the blood, apparently due to correction of enzymatic synthesis links and biotransformation of monoamines.
[Mh] Termos MeSH primário: Adamantano/análogos & derivados
Ansiolíticos/farmacologia
Transtornos de Ansiedade/tratamento farmacológico
Benzimidazóis/farmacologia
Transtorno Depressivo/tratamento farmacológico
Morfolinas/farmacologia
[Mh] Termos MeSH secundário: Adamantano/farmacologia
Animais
Monoaminas Biogênicas/farmacologia
Seres Humanos
Masculino
Ratos
Ratos Wistar
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-((2-morpholino)ethylthio)-5-ethoxybenzimidazole); 0 (Anti-Anxiety Agents); 0 (Benzimidazoles); 0 (Biogenic Monoamines); 0 (Morpholines); 0 (N-(2-adamantyl)-N-p-bromophenylamine); PJY633525U (Adamantane)
[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:171206
[St] Status:MEDLINE


  4 / 19721 MEDLINE  
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[PMID]:28460066
[Au] Autor:Kim HR; Kang HN; Shim HS; Kim EY; Kim J; Kim DJ; Lee JG; Lee CY; Hong MH; Kim SM; Kim H; Pyo KH; Yun MR; Park HJ; Han JY; Youn HA; Ahn MJ; Paik S; Kim TM; Cho BC
[Ad] Endereço:Division of Medical Oncology, Yonsei Cancer Center, Yonsei University College of Medicine, Seoul.
[Ti] Título:Co-clinical trials demonstrate predictive biomarkers for dovitinib, an FGFR inhibitor, in lung squamous cell carcinoma.
[So] Source:Ann Oncol;28(6):1250-1259, 2017 Jun 01.
[Is] ISSN:1569-8041
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Background: We conducted co-clinical trials in patient-derived xenograft (PDX) models to identify predictive biomarkers for the multikinase inhibitor dovitinib in lung squamous cell carcinoma (LSCC). Methods: The PDX01-02 were established from LSCC patients enrolled in the phase II trial of dovitinib (NCT01861197) and PDX03-05 were established from LSCC patients receiving surgery. These five PDX tumors were subjected to in vivo test of dovitinib efficacy, whole exome sequencing and gene expression profiling. Results: The PDX tumors recapitulate histopathological properties and maintain genomic characteristics of originating tumors. Concordant with clinical outcomes of the trial enrolled-LSCC patients, dovitinib produced substantial tumor regression in PDX-01 and PDX-05, whereas it resulted in tumor progression in PDX-02. PDX-03 and -04 also displayed poor antitumor efficacy to dovitinib. Mutational and genome-wide copy number profiles revealed no correlation between genomic alterations of FGFR1-3 and sensitivity to dovitinib. Of note, gene expression profiles revealed differentially expressed genes including FGF3 and FGF19 between PDX-01 and 05 and PDX-02-04. Pathway analysis identified two FGFR signaling-related gene sets, FGFR ligand binding/activation and SHC-mediated cascade pathway were substantially up-regulated in PDX-01 and 05, compared with PDX-02-04. The comparison of gene expression profiles between dovitinib-sensitive versus -resistant lung cancer cell lines in the Cancer Cell Line Encyclopedia database also found that transcriptional activation of 18 key signaling components in FGFR pathways can predict the sensitivity to dovitinib both in cell lines and PDX tumors. These results highlight FGFR pathway activation as a key molecular determinant for sensitivity to dovitinib. Conclusions: FGFR gene expression signatures are predictors for the response to dovitinib in LSCC.
[Mh] Termos MeSH primário: Benzimidazóis/uso terapêutico
Biomarcadores/sangue
Carcinoma de Células Escamosas/tratamento farmacológico
Ensaios Clínicos como Assunto
Neoplasias Pulmonares/tratamento farmacológico
Quinolonas/uso terapêutico
Receptores de Fatores de Crescimento de Fibroblastos/antagonistas & inibidores
[Mh] Termos MeSH secundário: Carcinoma de Células Escamosas/genética
Seres Humanos
Neoplasias Pulmonares/genética
Mutação
Receptores de Fatores de Crescimento de Fibroblastos/metabolismo
Transdução de Sinais
Sequenciamento Completo do Exoma
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4-amino-5-fluoro-3-(5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl)quinolin-2(1H)-one); 0 (Benzimidazoles); 0 (Biomarkers); 0 (Quinolones); 0 (Receptors, Fibroblast Growth Factor)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170502
[St] Status:MEDLINE
[do] DOI:10.1093/annonc/mdx098


  5 / 19721 MEDLINE  
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[PMID]:29335205
[Au] Autor:Chen X; Huan X; Liu Q; Wang Y; He Q; Tan C; Chen Y; Ding J; Xu Y; Miao Z; Yang C
[Ad] Endereço:Synthetic Organic & Medicinal Chemistry Laboratory, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, No. 19A Yuquan Road, Beijing 100049, China.
[Ti] Título:Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors.
[So] Source:Eur J Med Chem;145:389-403, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:The nuclear protein poly(ADP-ribose) polymerases-1/2 (PARP-1/2) are involved in DNA repair damaged by endogenous or exogenous process. And PARP-1/2 inhibitors have been proved to be clinically efficacious for DNA repair deficient tumors in the past decade. We have developed a series of 4,5,6,7-tetrahydrothienopyridin-2-yl benzimidazole carboxamides as novel and potent PARP-1/2 inhibitors. The best compound resulted from this series is compound 27 which displays excellent PARP-1 and PARP-2 inhibitory activity with IC of 18 nM and 42 nM, respectively. Furthermore, it can selectively kill BRCA2 deficient V-C8 cells with a CC of 920 nM. In the MDA-MB-436 (BRCA-1 mutant) xenograft model, this compound was well tolerated and showed single-agent activity. Based on the results above, compound 27 has been selected as a lead candidate targeting PARP-1/2 and its preclinical characterization is also underway.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Benzimidazóis/farmacologia
Desenho de Drogas
Inibidores de Poli(ADP-Ribose) Polimerases/farmacologia
Poli(ADP-Ribose) Polimerases/metabolismo
[Mh] Termos MeSH secundário: Administração Oral
Animais
Antineoplásicos/administração & dosagem
Antineoplásicos/química
Benzimidazóis/administração & dosagem
Benzimidazóis/química
Peso Corporal/efeitos dos fármacos
Linhagem Celular
Proliferação Celular/efeitos dos fármacos
Cricetulus
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Camundongos
Modelos Moleculares
Estrutura Molecular
Neoplasias Experimentais/tratamento farmacológico
Neoplasias Experimentais/patologia
Inibidores de Poli(ADP-Ribose) Polimerases/administração & dosagem
Inibidores de Poli(ADP-Ribose) Polimerases/química
Relação Estrutura-Atividade
Termodinâmica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Benzimidazoles); 0 (Poly(ADP-ribose) Polymerase Inhibitors); EC 2.4.2.30 (Poly(ADP-ribose) Polymerases)
[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:180117
[St] Status:MEDLINE


  6 / 19721 MEDLINE  
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[PMID]:29316526
[Au] Autor:Galal SA; Khairat SHM; Ali HI; Shouman SA; Attia YM; Ali MM; Mahmoud AE; Abdel-Halim AH; Fyiad AA; Tabll A; El-Shenawy R; El Abd YS; Ramdan R; El Diwani HI
[Ad] Endereço:Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries, National Research Centre, Cairo, 12622, Egypt. Electronic address: sh12galal@hotmail.com.
[Ti] Título:Part II: New candidates of pyrazole-benzimidazole conjugates as checkpoint kinase 2 (Chk2) inhibitors.
[So] Source:Eur J Med Chem;144:859-873, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:The development of checkpoint kinase 2 (Chk2) inhibitors for the treatment of cancer has been an ongoing and attractive objective in drug discovery. In this study, twenty-one feasible pyrazole-benzimidazole conjugates were synthesized to study their effect against Chk2 activity using Checkpoint Kinase Assay. The antitumor activity of these compounds was investigated using SRB assay. A potentiation effect of the synthesized Chk2 inhibitors was also investigated using the genotoxic anticancer drugs cisplatin and doxorubicin on breast carcinoma, (ER+) cell line (MCF-7). In vivo Chk2 and antitumor activities of 8d as a single-agent, and in combination with doxorubicin, were evaluated in breast cancer bearing animals induced by N-methylnitrosourea. The effect of 8d alone and in combination with doxorubicin was also studied on cell-cycle phases of MCF-7 cells using flow cytometry analysis. The results revealed their potencies as Chk2 inhibitors with IC ranges from 9.95 to 65.07 nM. Generally the effect of cisplatin or doxorubicin was potentiated by the effect of most of the compounds that were studied. The in vivo results indicated that the combination of 8d and doxorubicin inhibited checkpoint kinase activity more than either doxorubicin or 8d alone. There was a positive correlation between checkpoint kinase inhibition and the improvement observed in histopathological features. Single dose treatment with doxorubicin or 8d produced S phase cell cycle arrest whereas their combination created cell cycle arrest at G2/M from 8% in case of doxorubicin to 51% in combination. Gold molecular modelling studies displayed a high correlation to the biological results.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Benzimidazóis/farmacologia
Quinase do Ponto de Checagem 2/antagonistas & inibidores
Inibidores de Proteínas Quinases/farmacologia
Pirazóis/farmacologia
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/síntese química
Antineoplásicos/química
Benzimidazóis/química
Ciclo Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Quinase do Ponto de Checagem 2/metabolismo
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Feminino
Seres Humanos
Simulação de Acoplamento Molecular
Estrutura Molecular
Inibidores de Proteínas Quinases/síntese química
Inibidores de Proteínas Quinases/química
Pirazóis/química
Ratos
Ratos Sprague-Dawley
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Benzimidazoles); 0 (Protein Kinase Inhibitors); 0 (Pyrazoles); 3QD5KJZ7ZJ (pyrazole); E24GX49LD8 (benzimidazole); EC 2.7.1.11 (Checkpoint Kinase 2); EC 2.7.11.1 (CHEK2 protein, human)
[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:180110
[St] Status:MEDLINE


  7 / 19721 MEDLINE  
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[PMID]:29324623
[Au] Autor:Hussar DA
[Ad] Endereço:Remington Professor of Pharmacy Philadelphia College of Pharmacy University of the Sciences Philadelphia, Pa.
[Ti] Título:New Drugs 2018, part 1.
[So] Source:Nursing;48(2):36-44, 2018 Feb.
[Is] ISSN:1538-8689
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Aprovação de Drogas
[Mh] Termos MeSH secundário: Anticorpos Monoclonais/uso terapêutico
Anticorpos Neutralizantes/uso terapêutico
Antipirina/análogos & derivados
Antipirina/uso terapêutico
Benzamidas/uso terapêutico
Benzimidazóis/uso terapêutico
Carbamatos/uso terapêutico
Combinação de Medicamentos
Compostos Heterocíclicos de 4 ou mais Anéis/uso terapêutico
Seres Humanos
Compostos Macrocíclicos/uso terapêutico
Naltrexona/análogos & derivados
Naltrexona/uso terapêutico
Peptídeos Natriuréticos/uso terapêutico
Piridinas/uso terapêutico
Quinoxalinas/uso terapêutico
Sofosbuvir/uso terapêutico
Sulfonamidas/uso terapêutico
Estados Unidos
United States Food and Drug Administration
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ABT-493); 0 (Antibodies, Monoclonal); 0 (Antibodies, Neutralizing); 0 (Benzamides); 0 (Benzimidazoles); 0 (Carbamates); 0 (Drug Combinations); 0 (Heterocyclic Compounds, 4 or More Rings); 0 (Macrocyclic Compounds); 0 (Natriuretic Peptides); 0 (Pyridines); 0 (Quinoxalines); 0 (Sulfonamides); 0 (bezlotoxumab); 0 (naldemedine); 0 (pibrentasvir); 0 (voxilaprevir); 5S6W795CQM (Naltrexone); 74RWP7W0J9 (betrixaban); 7IK8Z952OK (plecanatide); KCU0C7RS7Z (velpatasvir); S798V6YJRP (phenylmethylpyrazolone); T3CHA1B51H (Antipyrine); WJ6CA3ZU8B (Sofosbuvir)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:N
[Da] Data de entrada para processamento:180112
[St] Status:MEDLINE
[do] DOI:10.1097/01.NURSE.0000529803.83288.e1


  8 / 19721 MEDLINE  
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[PMID]:29288939
[Au] Autor:Cheong JE; Zaffagni M; Chung I; Xu Y; Wang Y; Jernigan FE; Zetter BR; Sun L
[Ad] Endereço:Center for Drug Discovery and Translational Research, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02215, USA.
[Ti] Título:Synthesis and anticancer activity of novel water soluble benzimidazole carbamates.
[So] Source:Eur J Med Chem;144:372-385, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Metastases account for more than 90% of all cancer deaths and respond poorly to most therapies. There remains an urgent need for new therapeutic modalities for the treatment of advanced metastatic cancers. The benzimidazole methylcarbamate drugs, commonly used as anti-helmitics, have been suggested to have anticancer activity, but progress has been stalled by their poor water solubility and poor suitability for systemic delivery to disseminated cancers. We synthesized and characterized the anticancer activity of novel benzimidazoles containing an oxetane or an amine group to enhance solubility. Among them, the novel oxetanyl substituted compound 18 demonstrated significant cytotoxicity toward a variety of cancer cell types including prostate, lung, and ovarian cancers with strong activity toward highly aggressive cancer lines (IC : 0.9-3.8 µM). Compound 18 achieved aqueous solubility of 361 µM. In a mouse xenograft model of a highly metastatic human prostate cancer, compound 18 (30 mg/kg) significantly inhibited the growth of established tumors (T/C: 0.36) without noticeable toxicity.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Benzimidazóis/farmacologia
Carbamatos/farmacologia
Água/química
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/síntese química
Antineoplásicos/química
Benzimidazóis/síntese química
Benzimidazóis/química
Carbamatos/síntese química
Carbamatos/química
Proliferação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Seres Humanos
Masculino
Camundongos
Simulação de Acoplamento Molecular
Estrutura Molecular
Neoplasias Experimentais/tratamento farmacológico
Neoplasias Experimentais/patologia
Solubilidade
Relação Estrutura-Atividade
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Benzimidazoles); 0 (Carbamates); 059QF0KO0R (Water)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171231
[St] Status:MEDLINE


  9 / 19721 MEDLINE  
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[PMID]:29306026
[Au] Autor:So EC; Wu SN; Lo YC; Su K
[Ad] Endereço:Department of Anesthesia, An Nan Hospital, China Medical University, 70965, Tainan City, Taiwan; Department of Anesthesia, China Medical University, 40447 Taichung City, Taiwan. Electronic address: d11320@mail.tmanh.org.tw.
[Ti] Título:Differential regulation of tefluthrin and telmisartan on the gating charges of I activation and inactivation as well as on resurgent and persistent I in a pituitary cell line (GH ).
[So] Source:Toxicol Lett;285:104-112, 2018 Mar 15.
[Is] ISSN:1879-3169
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Voltage-gated Na currents (I ), known to contain many components (e.g., transient, resurgent and persistent I ) with unique gating properties, are involved in the generation and propagation of action potentials in excitable cells. In this study, how tefluthrin (Tef), a synthetic pyrethoid, and telmisartan (TEL), blocker of angiotensin II receptors can perturb those components of I was investigated. The presence of either Tef or TEL increased the values of the gating charges of I involved in the activation (z ) and inactivation (z ). Tef also increased the amplitude of resurgent I (I ) or persistent I (I ) in a pituitary cell line (GH ), while TEL produced minimal effects on them. Subsequent addition of either ranolazine (a blocker of late I ) or d-limonene (a monoterpene), could reverse the changes by TEL or Tef on z or z . In SCN5A-expressing HEK293T cells, addition of Tef or TEL also increased the peak amplitude and the inactivation time constant of I which was accompanied by the increased z value of I . Taken together, the results indicated that Tef- or TEL-mediated changes in the gating kinetics of I are linked to their actions on functional activity of neurons, neuroendocrine or endocrine cells.
[Mh] Termos MeSH primário: Benzimidazóis/farmacologia
Benzoatos/farmacologia
Ciclopropanos/farmacologia
Hidrocarbonetos Fluorados/farmacologia
Ativação do Canal Iônico/efeitos dos fármacos
Somatotrofos/efeitos dos fármacos
Canais de Sódio Disparados por Voltagem/metabolismo
[Mh] Termos MeSH secundário: Potenciais de Ação/efeitos dos fármacos
Animais
Linhagem Celular Tumoral
Cicloexenos/farmacologia
Células HEK293
Seres Humanos
Canal de Sódio Disparado por Voltagem NAV1.5/genética
Canal de Sódio Disparado por Voltagem NAV1.5/metabolismo
Ranolazina/farmacologia
Ratos
Somatotrofos/metabolismo
Terpenos/farmacologia
Transfecção
Canais de Sódio Disparados por Voltagem/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzimidazoles); 0 (Benzoates); 0 (Cyclohexenes); 0 (Cyclopropanes); 0 (Hydrocarbons, Fluorinated); 0 (NAV1.5 Voltage-Gated Sodium Channel); 0 (SCN5A protein, human); 0 (Terpenes); 0 (Voltage-Gated Sodium Channels); 2HE8P42H2J (2,3,5,6-tetrafluoro-4-methylbenzyl (Z)-(1RS)-cis-3-(2-chloro-3,3,3-trifluoroprop-1-enyl)-2,2-dimethylcyclopropanecarboxylate); 9MC3I34447 (limonene); A6IEZ5M406 (Ranolazine); U5SYW473RQ (telmisartan)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180219
[Lr] Data última revisão:
180219
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180107
[St] Status:MEDLINE


  10 / 19721 MEDLINE  
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[PMID]:29287783
[Au] Autor:da Silva Mansano N; Jorge IF; Chies AB; Viani GA; Spadella MA
[Ad] Endereço:Marília Medical School, Marília, São Paulo, Brazil. Electronic address: maspadella@famema.br.
[Ti] Título:Effects of telmisartan and losartan on irradiated testes.
[So] Source:Life Sci;194:157-167, 2018 Feb 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: To analyze the effects of radiation on the reproductive tissue of male Wistar rats and to evaluate whether treatment with the Ang II AT1 receptor antagonists telmisartan and losartan mitigate the dysfunctions resulting from this exposure. MAIN METHODS: Rats were randomly divided into groups: Control, Irradiated, Telmisartan, Losartan, Irradiated+Telmisartan, and Irradiated+Losartan. Single dose of 5Gy was administered directly into the scrotum, followed by treatment with telmisartan (12mg/kg/day) or losartan (34mg/kg/two times/day) for 60days. Testicular function parameters were evaluated from spermatozoa of the vas deferens. Testes were processed for histopathological and morphometric-stereological analysis. Proliferating cell nuclear antigen (PCNA) immunohistochemistry was evaluated. KEY FINDINGS: Radiation significantly reduced sperm motility, concentration, vitality, and increased the number of abnormal spermatozoa. Telmisartan and losartan did not significantly prevent these radiation-induced disorders. Seminiferous tubules were atrophied in both untreated and treated irradiated testes, and exhibited vacuoles, increased interstitial tissue and high number of blood vessels. However, several seminiferous tubules in recuperation were founded among damaged tubules in the testes of treated animals. The PCNA immunohistochemistry confirmed these outcomes. PCNA-positive cells were detected in dividing spermatogonia and spermatocytes from irradiated telmisartan and losartan treated rats whereas in the only-irradiated group, PCNA staining was observed in the nuclei of only the surviving spermatogonia. SIGNIFICANCE: Under these experimental conditions, the testicular function parameters showed that radiation produced marked damage that was not reversed by treatments. However, gonadal restructuring and recovery of spermatogenesis in treated animals may to reflect attenuation of radiation-induced damages and potential start of recovery.
[Mh] Termos MeSH primário: Bloqueadores do Receptor Tipo 1 de Angiotensina II/farmacologia
Benzimidazóis/farmacologia
Benzoatos/farmacologia
Losartan/farmacologia
Protetores contra Radiação/farmacologia
Testículo/efeitos dos fármacos
Testículo/efeitos da radiação
[Mh] Termos MeSH secundário: Animais
Masculino
Ratos Wistar
Espermatogênese/efeitos dos fármacos
Espermatogênese/efeitos da radiação
Espermatozoides/efeitos dos fármacos
Espermatozoides/patologia
Espermatozoides/efeitos da radiação
Testículo/patologia
Testículo/fisiopatologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Angiotensin II Type 1 Receptor Blockers); 0 (Benzimidazoles); 0 (Benzoates); 0 (Radiation-Protective Agents); JMS50MPO89 (Losartan); U5SYW473RQ (telmisartan)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180213
[Lr] Data última revisão:
180213
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171231
[St] Status:MEDLINE



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