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Pesquisa : G07.690.773.984.300 [Categoria DeCS]
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[PMID]:29396713
[Au] Autor:Kiladjian JJ; Guglielmelli P; Griesshammer M; Saydam G; Masszi T; Durrant S; Passamonti F; Jones M; Zhen H; Li J; Gadbaw B; Perez Ronco J; Khan M; Verstovsek S
[Ad] Endereço:Centre d'Investigations Cliniques (CIC1427), Hôpital Saint-Louis, AP-HP, INSERM, CLIP2 "Saint-Louis - Paris Nord," Early Phase Research Center, Université Paris Diderot, 1, Avenue Claude Vellefaux, 75010, Paris, France. jean-jacques.kiladjian@aphp.fr.
[Ti] Título:Efficacy and safety of ruxolitinib after and versus interferon use in the RESPONSE studies.
[So] Source:Ann Hematol;97(4):617-627, 2018 Apr.
[Is] ISSN:1432-0584
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Ruxolitinib was well tolerated and superior to best available therapy (including interferon [IFN]) in controlling hematocrit without phlebotomy eligibility, normalizing blood counts, and improving polycythemia vera-related symptoms in the Study of Efficacy and Safety in Polycythemia Vera Subjects Who Are Resistant to or Intolerant of Hydroxyurea: JAK Inhibitor INC424 (INCB018424) Tablets Versus Best Available Care (RESPONSE) studies. This ad hoc analysis focuses on ruxolitinib in relation to IFN in the RESPONSE studies, with attention on the following: (1) safety and efficacy of ruxolitinib and best available therapy in patients who received IFN before study randomization, (2) safety and efficacy of IFN during randomized treatment in best available therapy arm, and (3) use of ruxolitinib after crossover from best available therapy in IFN-treated patients. IFN exposure before randomization had little effect on the efficacy or safety of ruxolitinib. In the randomized treatment arms, ruxolitinib was superior to IFN in efficacy [hematocrit control (RESPONSE = 60% of ruxolitinib vs 23% of IFN patients; RESPONSE-2 = 62% of ruxolitinib vs 15% of IFN patients)] and was tolerated better in hydroxyurea-resistant or hydroxyurea-intolerant patients. After crossing over to receive ruxolitinib, patients who had initially received IFN and did not respond had improved hematologic and spleen responses (62% of patients at any time after crossover) and an overall reduction in phlebotomy procedures. Rates and incidences of the most common adverse events decreased after crossover to ruxolitinib, except for infections (primarily grade 1 or 2). These data suggest that ruxolitinib is efficacious and well tolerated in patients who were previously treated with IFN. The RESPONSE (NCT01243944) and RESPONSE-2 (NCT02038036) studies were registered at clinicaltrials.gov .
[Mh] Termos MeSH primário: Antineoplásicos/uso terapêutico
Interferons/uso terapêutico
Janus Quinases/antagonistas & inibidores
Policitemia Vera/tratamento farmacológico
Inibidores de Proteínas Quinases/uso terapêutico
Pirazóis/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Idoso
Antineoplásicos/efeitos adversos
Sangria/efeitos adversos
Terapia Combinada/efeitos adversos
Estudos Cross-Over
Monitoramento de Medicamentos
Resistência a Múltiplos Medicamentos
Resistência a Medicamentos Antineoplásicos
Feminino
Seres Humanos
Hidroxiureia/efeitos adversos
Hidroxiureia/uso terapêutico
Interferons/efeitos adversos
Janus Quinases/metabolismo
Masculino
Meia-Idade
Policitemia Vera/metabolismo
Policitemia Vera/fisiopatologia
Policitemia Vera/terapia
Padrões de Prática Médica
Inibidores de Proteínas Quinases/efeitos adversos
Pirazóis/efeitos adversos
Reprodutibilidade dos Testes
Esplenomegalia/etiologia
Esplenomegalia/prevenção & controle
[Pt] Tipo de publicação:CLINICAL TRIAL; CLINICAL TRIAL, PHASE III; COMPARATIVE STUDY; EQUIVALENCE TRIAL; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (INCB018424); 0 (Protein Kinase Inhibitors); 0 (Pyrazoles); 9008-11-1 (Interferons); EC 2.7.10.2 (Janus Kinases); X6Q56QN5QC (Hydroxyurea)
[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:180204
[Cl] Clinical Trial:ClinicalTrial
[St] Status:MEDLINE
[do] DOI:10.1007/s00277-017-3225-1


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[PMID]:29332223
[Au] Autor:Togasaki E; Shimizu N; Nagao Y; Kawajiri-Manako C; Shimizu R; Oshima-Hasegawa N; Muto T; Tsukamoto S; Mitsukawa S; Takeda Y; Mimura N; Ohwada C; Takeuchi M; Sakaida E; Iseki T; Yoshitomi H; Ohtsuka M; Miyazaki M; Nakaseko C
[Ad] Endereço:Department of Hematology, Chiba University Hospital, 1-8-1 Inohana, Chuo-ku, Chiba, 260-8677, Japan.
[Ti] Título:Long-term efficacy of partial splenic embolization for the treatment of steroid-resistant chronic immune thrombocytopenia.
[So] Source:Ann Hematol;97(4):655-662, 2018 Apr.
[Is] ISSN:1432-0584
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Thrombopoietin-receptor agonists have been recently introduced for a second-line treatment of immune thrombocytopenia (ITP). Splenectomy has tended to be avoided because of its complications, but the response rate of splenectomy is 60-80% and it has still been considered for steroid-refractory ITP. We performed partial splenic embolization (PSE) as an alternative to splenectomy. Between 1988 and 2013, 91 patients with steroid-resistant ITP underwent PSE at our hospital, and we retrospectively analyzed the efficacy and long-term outcomes of PSE. The complete response rate (CR, platelets > 100 × 10 /L) was 51% (n = 46), and the overall response rate (CR plus response (R), > 30 × 10 /L) was 84% (n = 76). One year after PSE, 70% of patients remained CR and R. The group with peak platelet count after PSE ≥ 300 × 10 /L (n = 29) exhibited a significantly higher platelet count than the group with platelet count < 300 × 10 /L (n = 40) at any time point after PSE. The failure-free survival (FFS) rates at 1, 5, and 10 years were 78, 56, and 52%, respectively. Second PSE was performed in 20 patients who relapsed (n = 14) or had no response to the initial PSE (n = 6), and the overall response was achieved in 63% patients. There were no PSE-related deaths. These results indicate that PSE is a safe and effective alternative therapy to splenectomy for patients with steroid-resistant ITP as it generates long-term, durable responses.
[Mh] Termos MeSH primário: Embolização Terapêutica
Púrpura Trombocitopênica Idiopática/terapia
Baço/irrigação sanguínea
[Mh] Termos MeSH secundário: Adolescente
Corticosteroides/uso terapêutico
Adulto
Idoso
Idoso de 80 Anos ou mais
Intervalo Livre de Doença
Resistência a Medicamentos
Resistência a Múltiplos Medicamentos
Embolização Terapêutica/efeitos adversos
Feminino
Seguimentos
Hospitais Universitários
Seres Humanos
Japão
Masculino
Meia-Idade
Tamanho do Órgão
Púrpura Trombocitopênica Idiopática/diagnóstico por imagem
Púrpura Trombocitopênica Idiopática/tratamento farmacológico
Púrpura Trombocitopênica Idiopática/patologia
Estudos Retrospectivos
Baço/diagnóstico por imagem
Baço/efeitos dos fármacos
Baço/patologia
Esteroides/uso terapêutico
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; OBSERVATIONAL STUDY
[Nm] Nome de substância:
0 (Adrenal Cortex Hormones); 0 (Steroids)
[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:180115
[St] Status:MEDLINE
[do] DOI:10.1007/s00277-018-3232-x


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[PMID]:29322203
[Au] Autor:Dada R
[Ad] Endereço:Department of Oncology MBC J-64, King Faisal Specialist Hospital and Research Center, P.O. Box 40047, Jeddah, 21499, Kingdom of Saudi Arabia. rdada@kfshrc.edu.sa.
[Ti] Título:Program death inhibitors in classical Hodgkin's lymphoma: a comprehensive review.
[So] Source:Ann Hematol;97(4):555-561, 2018 Apr.
[Is] ISSN:1432-0584
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Cancer cells are able to induce immune system tolerance through different mechanisms. Recent achievements in the understanding of tumor microenvironment, invasion, and metastasizing have contributed to accelerated drug developments and approvals. Hodgkin lymphoma (HL) cells are the minority in a lymphocyte-rich microenvironment of HL tissue. The program death-1 (PD-1)/PD-ligand-1 checkpoint is one of the known effective pathways in classical HL to escape the immune system cells. The approval of PD-1 inhibitors in different cancer types with exciting response rates is truly revolutionizing our treatment armamentarium against cancer in general and classical HL in specific. Although the disease is one of the most curable tumors, we still need better outcome with more gentle treatment, especially for relapsed and refractory (r/r) patients. In this article, we review the current literature on immune checkpoint inhibitors and currently ongoing studies with nivolumab and pembrolizumab in r/r classical HL.
[Mh] Termos MeSH primário: Antineoplásicos/uso terapêutico
Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico
Antígeno B7-H1/antagonistas & inibidores
Doença de Hodgkin/tratamento farmacológico
Proteínas de Neoplasias/antagonistas & inibidores
Receptor de Morte Celular Programada 1/antagonistas & inibidores
[Mh] Termos MeSH secundário: Anticorpos Monoclonais/efeitos adversos
Anticorpos Monoclonais/uso terapêutico
Anticorpos Monoclonais Humanizados/efeitos adversos
Anticorpos Monoclonais Humanizados/uso terapêutico
Antineoplásicos/efeitos adversos
Antineoplásicos Imunológicos/efeitos adversos
Antineoplásicos Imunológicos/uso terapêutico
Protocolos de Quimioterapia Combinada Antineoplásica/efeitos adversos
Antígeno B7-H1/metabolismo
Aprovação de Drogas
Resistência a Múltiplos Medicamentos
Resistência a Medicamentos Antineoplásicos
Doença de Hodgkin/metabolismo
Seres Humanos
Terapia de Alvo Molecular/efeitos adversos
Proteínas de Neoplasias/metabolismo
Receptor de Morte Celular Programada 1/metabolismo
Qualidade de Vida
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antibodies, Monoclonal); 0 (Antibodies, Monoclonal, Humanized); 0 (Antineoplastic Agents); 0 (Antineoplastic Agents, Immunological); 0 (B7-H1 Antigen); 0 (CD274 protein, human); 0 (Neoplasm Proteins); 0 (PDCD1 protein, human); 0 (Programmed Cell Death 1 Receptor); 31YO63LBSN (nivolumab); DPT0O3T46P (pembrolizumab)
[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:10.1007/s00277-017-3226-0


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[PMID]:28452902
[Au] Autor:Fan KY; Liu HC
[Ad] Endereço:*Department of Psychiatry, Taipei City Psychiatric Center, Taipei City Hospital; and †Department of Psychiatry, School of Medicine, Taipei Medical University, Taipei, Taiwan.
[Ti] Título:Delirium Associated With Fluoxetine Discontinuation: A Case Report.
[So] Source:Clin Neuropharmacol;40(3):152-153, 2017 May/Jun.
[Is] ISSN:1537-162X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Withdrawal symptoms on selective serotonin reuptake inhibitor (SSRI) discontinuation have raised clinical attention increasingly. However, delirium is rarely reported in the SSRI discontinuation syndrome. CASE: We report a case of delirium developing after fluoxetine discontinuation in a 65-year-old female patient with major depressive disorder. She experienced psychotic depression with limited response to treatment of fluoxetine 40 mg/d and quetiapine 100 mg/d for 3 months. After admission, we tapered fluoxetine gradually in 5 days because of its limited effect. However, delirious pictures developed 2 days after we stopped fluoxetine. Three days later, we added back fluoxetine 10 mg/d. Her delirious features gradually improved, and the clinical presentation turned into previous psychotic depression state. We gradually increased the medication to fluoxetine 60 mg/d and olanzapine 20 mg/d in the following 3 weeks. Her psychotic symptoms decreased, and there has been no delirious picture noted thereafter. CONCLUSIONS: Delirium associated with fluoxetine discontinuation is a much rarer complication in SSRI discontinuation syndrome. The symptoms of SSRI discontinuation syndrome may be attributable to a rapid decrease in serotonin availability. In general, the shorter the half-life of any medication, the greater the likelihood patients will experience discontinuation symptoms. Genetic vulnerability might be a potential factor to explain that SSRI discontinuation syndrome also occurred rapidly in people taking long-half-life fluoxetine. The genetic polymorphisms of both pharmacokinetic and pharmacodynamic pathways might be potentially associated with SSRI discontinuation syndrome.
[Mh] Termos MeSH primário: Antidepressivos de Segunda Geração/efeitos adversos
Delírio/etiologia
Fluoxetina/efeitos adversos
Inibidores da Captação de Serotonina/efeitos adversos
Síndrome de Abstinência a Substâncias/etiologia
[Mh] Termos MeSH secundário: Idoso
Antipsicóticos/uso terapêutico
Benzodiazepinas/uso terapêutico
Delírio/prevenção & controle
Transtorno Depressivo Maior/tratamento farmacológico
Monitoramento de Medicamentos
Resistência a Múltiplos Medicamentos
Quimioterapia Combinada
Feminino
Fluoxetina/uso terapêutico
Seres Humanos
Inibidores da Captação de Serotonina/uso terapêutico
Síndrome de Abstinência a Substâncias/fisiopatologia
Síndrome de Abstinência a Substâncias/prevenção & controle
Resultado do Tratamento
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antidepressive Agents, Second-Generation); 0 (Antipsychotic Agents); 0 (Serotonin Uptake Inhibitors); 01K63SUP8D (Fluoxetine); 12794-10-4 (Benzodiazepines); N7U69T4SZR (olanzapine)
[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:170429
[St] Status:MEDLINE
[do] DOI:10.1097/WNF.0000000000000214


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[PMID]:29180864
[Au] Autor:Shi J; Su Y; Liu W; Chang J; Zhang Z
[Ad] Endereço:School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou.
[Ti] Título:A nanoliposome-based photoactivable drug delivery system for enhanced cancer therapy and overcoming treatment resistance.
[So] Source:Int J Nanomedicine;12:8257-8275, 2017.
[Is] ISSN:1178-2013
[Cp] País de publicação:New Zealand
[La] Idioma:eng
[Ab] Resumo:Recently, stimuli-responsive drug delivery systems (DDSs) with high spatial/temporal resolution bring many benefits to cancer treatment. However, cancer cells always develop ways to resist and evade treatment, ultimately limit the treatment efficacy of the DDSs. Here, we introduce photo-activated nanoliposomes (PNLs) that impart light-induced cytotoxicity and reversal of drug resistance in synchrony with a photoinitiated and rapid release of antitumor drug. The PNLs consist of a nanoliposome doped with a photosensitizer (hematoporphyrin monomethyl ether [HMME]) in the lipid bilayer and an antitumor drug doxorubicin (DOX) encapsulated inside. PNLs have several distinctive capabilities: 1) carrying high loadings of DOX and HMME and releasing the payloads in a photo-cleavage manner with high spatial/temporal resolution at the site of actions via photocatalysis; 2) reducing drug efflux in MCF-7/multidrug resistance cells via decreasing the level of P-glycoprotein induced by photodynamic therapy (PDT); 3) accumulating in tumor site taking advantage of the enhanced permeability and retention effect; and 4) combining effective chemotherapy and PDT to exert much enhanced anticancer effect and achieving significant tumor regression in a drug-resistant tumor model with little side effects.
[Mh] Termos MeSH primário: Antineoplásicos/administração & dosagem
Sistemas de Liberação de Medicamentos/métodos
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Lipossomos/administração & dosagem
Fotoquimioterapia/métodos
[Mh] Termos MeSH secundário: Subfamília B de Transportador de Cassetes de Ligação de ATP/metabolismo
Animais
Antineoplásicos/farmacologia
Doxorrubicina/administração & dosagem
Doxorrubicina/farmacologia
Resistência a Múltiplos Medicamentos/efeitos dos fármacos
Feminino
Hematoporfirinas/química
Hematoporfirinas/farmacologia
Seres Humanos
Bicamadas Lipídicas/química
Lipossomos/química
Lipossomos/farmacologia
Células MCF-7
Camundongos Endogâmicos BALB C
Nanoestruturas/administração & dosagem
Nanoestruturas/química
Fármacos Fotossensibilizantes/farmacologia
Espécies Reativas de Oxigênio/metabolismo
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ABCB1 protein, human); 0 (ATP Binding Cassette Transporter, Sub-Family B); 0 (Antineoplastic Agents); 0 (Hematoporphyrins); 0 (Lipid Bilayers); 0 (Liposomes); 0 (Photosensitizing Agents); 0 (Reactive Oxygen Species); 0 (hematoporphyrin monomethyl ether); 80168379AG (Doxorubicin)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171129
[St] Status:MEDLINE
[do] DOI:10.2147/IJN.S143776


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[PMID]:29335204
[Au] Autor:Gu X; Jiang Y; Qu Y; Chen J; Feng D; Li C; Yin X
[Ad] Endereço:Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Jiangsu Center for the Collaboration and Innovation of Cancer Biotherapy, Xuzhou Medical University, Xuzhou 221004, People's Republic of China.
[Ti] Título:Synthesis and biological evaluation of bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potential P-glycoprotein and tumor metastasis inhibitors.
[So] Source:Eur J Med Chem;145:379-388, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:As a continuation of previous research, fifteen bifendate derivatives bearing 6,7-dihydro-dibenzo [c,e]azepine scaffold were synthesized and evaluated as P-gp-medicated multidrug resistance (MDR) reversal agents. Biological evaluation indicated that compounds 6k and 9c more potently reversed P-gp-mediated MDR than bifendate and verapamil (VRP) by blocking P-gp mediated drug efflux function and not by decreasing P-gp expression in K562/A02 MDR cells. Interestingly, wound-healing and chamber migration assay showed that 6k and 9c could significantly attenuate the migration of MDA-MB-231 cells. Notably, 6k and 9c could markedly suppress the invasive activity of MDA-MB-231 cells, thus displayed potential anti-metastasis activity. Preliminary mechanism studies indicated that the anti-metastasis activity of 6k and 9c was associated with their inhibitory effect on the activity and expression of MMP-2 and MMP-9. These results, together with the MDR reversal results indicated that compounds 6k and 9c might be promising leads for developing novel anti-cancer agents with P-gp and tumor metastasis inhibitory activities.
[Mh] Termos MeSH primário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/antagonistas & inibidores
Antineoplásicos/farmacologia
Azepinas/farmacologia
Compostos de Bifenilo/farmacologia
Neoplasias/tratamento farmacológico
[Mh] Termos MeSH secundário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo
Antineoplásicos/síntese química
Antineoplásicos/química
Azepinas/química
Compostos de Bifenilo/síntese química
Compostos de Bifenilo/química
Linhagem Celular Tumoral
Relação Dose-Resposta a Droga
Resistência a Múltiplos Medicamentos/efeitos dos fármacos
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Células K562
Estrutura Molecular
Neoplasias/metabolismo
Neoplasias/patologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Antineoplastic Agents); 0 (Azepines); 0 (Biphenyl Compounds); 0G32E321W1 (bifendate)
[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


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[PMID]:29291440
[Au] Autor:Vágvölgyi M; Martins A; Kulmány Á; Zupkó I; Gáti T; Simon A; Tóth G; Hunyadi A
[Ad] Endereço:Institute of Pharmacognosy, Faculty of Pharmacy, University of Szeged, Szeged, Hungary.
[Ti] Título:Nitrogen-containing ecdysteroid derivatives vs. multi-drug resistance in cancer: Preparation and antitumor activity of oximes, oxime ethers and a lactam.
[So] Source:Eur J Med Chem;144:730-739, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Multidrug resistance is a widespread problem among various diseases and cancer is no exception. We had previously described the chemo-sensitizing activity of ecdysteroid derivatives with low polarity on drug susceptible and multi-drug resistant (MDR) cancer cells. We have also shown that these molecules have a marked selectivity towards the MDR cells. Recent studies on the oximation of various steroid derivatives indicated remarkable increase in their antitumor activity, but there is no related bioactivity data on ecdysteroid oximes. In our present study, 13 novel ecdysteroid derivatives (oximes, oxime ethers and a lactam) and one known compound were synthesized from 20-hydroxyecdysone 2,3;20,22-diacetonide and fully characterized by comprehensive NMR techniques revealing their complete H and C signal assignments. The compounds exerted moderate to strong in vitro antiproliferative activity on HeLa, SiHa, MCF-7 and MDA-MB-231 cell lines. Oxime and particularly oxime ether formation strongly increased their inhibitory activity on the efflux of rhodamine 123 by P-glycoprotein (P-gp), while the new ecdysteroid lactam did not interfere with the efflux function. All compounds exerted potent chemo-sensitizing activity towards doxorubicin on a mouse lymphoma cell line and on its MDR counterpart, and, on the latter, the lactam was found the most active. Because of its MDR-selective chemo-sensitizing activity with no functional effect on P-gp, this lactam is of high potential interest as a new lead for further antitumor studies.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Ecdisteroides/farmacologia
Éteres/farmacologia
Lactamas/farmacologia
Neoplasias/tratamento farmacológico
Nitrogênio/farmacologia
Oximas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Resistência a Múltiplos Medicamentos/efeitos dos fármacos
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Ensaios de Seleção de Medicamentos Antitumorais
Ecdisteroides/síntese química
Ecdisteroides/química
Éteres/síntese química
Éteres/química
Seres Humanos
Lactamas/síntese química
Lactamas/química
Estrutura Molecular
Neoplasias/patologia
Nitrogênio/química
Oximas/síntese química
Oximas/química
Relação Estrutura-Atividade
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Ecdysteroids); 0 (Ethers); 0 (Lactams); 0 (Oximes); N762921K75 (Nitrogen)
[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]:29326268
[Au] Autor:Cowell AN; Istvan ES; Lukens AK; Gomez-Lorenzo MG; Vanaerschot M; Sakata-Kato T; Flannery EL; Magistrado P; Owen E; Abraham M; LaMonte G; Painter HJ; Williams RM; Franco V; Linares M; Arriaga I; Bopp S; Corey VC; Gnädig NF; Coburn-Flynn O; Reimer C; Gupta P; Murithi JM; Moura PA; Fuchs O; Sasaki E; Kim SW; Teng CH; Wang LT; Akidil A; Adjalley S; Willis PA; Siegel D; Tanaseichuk O; Zhong Y; Zhou Y; Llinás M; Ottilie S; Gamo FJ; Lee MCS; Goldberg DE; Fidock DA; Wirth DF; Winzeler EA
[Ad] Endereço:School of Medicine, University of California San Diego (UCSD), 9500 Gilman Drive, La Jolla, CA 92093, USA.
[Ti] Título:Mapping the malaria parasite druggable genome by using in vitro evolution and chemogenomics.
[So] Source:Science;359(6372):191-199, 2018 01 12.
[Is] ISSN:1095-9203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Chemogenetic characterization through in vitro evolution combined with whole-genome analysis can identify antimalarial drug targets and drug-resistance genes. We performed a genome analysis of 262 parasites resistant to 37 diverse compounds. We found 159 gene amplifications and 148 nonsynonymous changes in 83 genes associated with drug-resistance acquisition, where gene amplifications contributed to one-third of resistance acquisition events. Beyond confirming previously identified multidrug-resistance mechanisms, we discovered hitherto unrecognized drug target-inhibitor pairs, including thymidylate synthase and a benzoquinazolinone, farnesyltransferase and a pyrimidinedione, and a dipeptidylpeptidase and an arylurea. This exploration of the resistome and druggable genome will likely guide drug discovery and structural biology efforts, while also advancing our understanding of resistance mechanisms available to the malaria parasite.
[Mh] Termos MeSH primário: Antimaláricos/farmacologia
Resistência a Medicamentos/genética
Genoma de Protozoário
Plasmodium falciparum/efeitos dos fármacos
Plasmodium falciparum/genética
[Mh] Termos MeSH secundário: Ativação Metabólica
Alelos
Variações do Número de Cópias de DNA
Evolução Molecular Direcionada
Resistência a Múltiplos Medicamentos/genética
Genes de Protozoários
Metabolômica
Mutação
Plasmodium falciparum/crescimento & desenvolvimento
Seleção Genética
Fatores de Transcrição/química
Fatores de Transcrição/genética
Fatores de Transcrição/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antimalarials); 0 (Transcription Factors)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180113
[St] Status:MEDLINE
[do] DOI:10.1126/science.aan4472


  9 / 13302 MEDLINE  
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[PMID]:29210765
[Au] Autor:Grota PG; Grant PS
[Ad] Endereço:Office of Faculty Affairs and Diversity, School of Nursing, University of Texas Health, San Antonio (Dr Grota); and Infection Prevention and Quality, Methodist Hospital for Surgery, Addison, Texas (Ms Grant).
[Ti] Título:Environmental Infection Prevention: Priorities of Patient Safety Collaboration.
[So] Source:Crit Care Nurs Q;41(1):38-46, 2018 Jan/Mar.
[Is] ISSN:1550-5111
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Although progress has been made in decreasing health care-associated infections (HAI) in intensive care unit (ICU) patients, there has been an increase in HAI caused by drug-resistant pathogens, particularly those that contaminate the environment such as methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus, Pseudomonas spp, Acinetobacter spp, and Clostridium difficile. The ICU environment including sinks and medical equipment has been identified as being at risk for contamination and associated with cross-transmission of pathogens between the health care provider, the environment, and the patient. This article addresses the role of the ICU nurse as a team facilitator collaborating with environmental services, infection preventionists, and others to influence ICU design during preconstruction planning and unit environmental hygiene after construction to promote patient safety and prevent HAI associated with contaminated environments and equipment.
[Mh] Termos MeSH primário: Enfermagem de Cuidados Críticos/normas
Infecção Hospitalar/prevenção & controle
Arquitetura Hospitalar/métodos
Controle de Infecções/métodos
Segurança do Paciente/normas
[Mh] Termos MeSH secundário: Infecção Hospitalar/transmissão
Resistência a Múltiplos Medicamentos
Pessoal de Saúde
Seres Humanos
Unidades de Terapia Intensiva/normas
Staphylococcus aureus Resistente à Meticilina/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:N
[Da] Data de entrada para processamento:171207
[St] Status:MEDLINE
[do] DOI:10.1097/CNQ.0000000000000184


  10 / 13302 MEDLINE  
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[PMID]:29233614
[Au] Autor:Paterna A; Khonkarn R; Mulhovo S; Moreno A; Madeira Girio P; Baubichon-Cortay H; Falson P; Ferreira MU
[Ad] Endereço:Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisbon, Portugal.
[Ti] Título:Monoterpene indole alkaloid azine derivatives as MDR reversal agents.
[So] Source:Bioorg Med Chem;26(2):421-434, 2018 01 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Aiming at generating a library of bioactive indole alkaloid derivatives as multidrug resistance (MDR) reversers, two epimeric indole alkaloids (1 and 2) were submitted to chemical transformations, giving rise to twenty-four derivatives (5-28), bearing new aromatic or aliphatic azine moieties. The structure of the compounds was established by 1D and 2D NMR (COSY, HMBC, HMQC and NOESY) experiments. Two different strategies were employed for assessing their anti-MDR potential, namely through the evaluation of their activity as inhibitors of typical MDR ABC transporters overexpressed by cell transfection, such as ABCB1 (P-gp), ABCC1 (MRP1), and ABCG2 (BCRP), or by evaluating their ability as collateral sensitivity (CS) agents in cells overexpressing MRP1. A considerable MDR reversing activity was observed for compounds bearing the aromatic azine moiety. The strongest and most selective P-gp inhibition was found for the epimeric azines 5 and 6, bearing a para-methylbenzylidene moiety. Instead, compounds 17 and 18 that possess a di-substituted benzylidene portion with methoxy and hydroxyl groups, selectively inhibited MRP1 drug-efflux. None of these compounds inhibited BCRP. Compounds 5, 6 and 18 were further investigated in drug combination experiments, which corroborated their anti-MDR potential. Moreover, it was observed that compound 12, with an aromatic azine moiety, and compounds 23-26, sharing a new aliphatic substituent, displayed a CS activity, selectively killing MRP1-overexpressing cells. Among these last compounds, it could be established that addition of 19, 23 and 25 to MRP1-overexpressing cells led to glutathione depletion triggering cell death through apoptosis.
[Mh] Termos MeSH primário: Alcaloides/farmacologia
Resistência a Múltiplos Medicamentos/efeitos dos fármacos
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Hidrazinas/farmacologia
Indóis/farmacologia
[Mh] Termos MeSH secundário: Alcaloides/síntese química
Alcaloides/química
Animais
Linhagem Celular
Proliferação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Cricetinae
Relação Dose-Resposta a Droga
Células HEK293
Seres Humanos
Hidrazinas/síntese química
Hidrazinas/química
Indóis/síntese química
Indóis/química
Camundongos
Estrutura Molecular
Células NIH 3T3
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Alkaloids); 0 (Hydrazines); 0 (Indoles)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180220
[Lr] Data última revisão:
180220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171214
[St] Status:MEDLINE



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