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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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[PMID]:29289881
[Au] Autor:Sathish M; Kavitha B; Nayak VL; Tangella Y; Ajitha A; Nekkanti S; Alarifi A; Shankaraiah N; Nagesh N; Kamal A
[Ad] Endereço:Medicinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
[Ti] Título:Synthesis of podophyllotoxin linked ß-carboline congeners as potential anticancer agents and DNA topoisomerase II inhibitors.
[So] Source:Eur J Med Chem;144:557-571, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A series of new podophyllotoxin linked ß-carboline congeners have been synthesized by coupling various substituted ß-carboline acids with 4ß-aminopodophyllotoxin. Evaluation of their anticancer activity against a panel of human cancer cell lines such as lung cancer (A549), prostate cancer (DU-145), MDA MB-231 (breast cancer), HT-29 (colon cancer) and HeLa (cervical cancer) suggested that 7i and 7j are the most cytotoxic compounds with IC values of 1.07 ±â€¯0.07 µM and 1.14 ±â€¯0.16 respectively against DU-145 cell line. Further, detailed biological studies such as cell cycle analysis, topoisomerase II inhibition, Comet assay, DNA binding studies and docking studies have revealed that these congeners are DNA interacting topoisomerase II inhibitors.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Carbolinas/farmacologia
DNA Topoisomerases Tipo II/metabolismo
Podofilotoxina/farmacologia
Inibidores da Topoisomerase II/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Carbolinas/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Simulação de Acoplamento Molecular
Estrutura Molecular
Podofilotoxina/química
Relação Estrutura-Atividade
Inibidores da Topoisomerase II/síntese química
Inibidores da Topoisomerase II/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Carbolines); 0 (Topoisomerase II Inhibitors); 94HMA1I78O (norharman); 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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[PMID]:29269253
[Au] Autor:Zhang X; Rakesh KP; Shantharam CS; Manukumar HM; Asiri AM; Marwani HM; Qin HL
[Ad] Endereço:Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan 430073, PR China.
[Ti] Título:Podophyllotoxin derivatives as an excellent anticancer aspirant for future chemotherapy: A key current imminent needs.
[So] Source:Bioorg Med Chem;26(2):340-355, 2018 01 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Cancer is one of the leading groups of threatened caused by abnormal state cell growth and second leading diseases involved in the major global death. To treat this, research looking for promising anticancer drugs from natural resource, or synthesized novel molecules by diverse group of scientists worldwide. Currently, drugs get into clinical practices and showing side effects with target actions which in turn leading to multidrug resistance unknowingly. Podophyllotoxin, a naturally occurring lignan and with hybrids have become one of the most attractive subjects due to their broad spectrum of pharmacological activities. Podophyllotoxin derivatives have been the centre of attention of extensive chemical amendment and pharmacological investigation in modern decades. Mainly, the innovation of the semi-synthetic anticancer drugs etoposide and teniposide has stimulated prolonged research interest in this structural phenotype. The present review focuses mainly onnew anticancer drugs from podophyllotoxin analogs, mechanism of action and their structure-activity relationships (SAR) as potential anticancer candidates for future discovery of suitable drug candidates.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Neoplasias/tratamento farmacológico
Podofilotoxina/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/química
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Seres Humanos
Estrutura Molecular
Neoplasias/patologia
Podofilotoxina/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Antineoplastic Agents); L36H50F353 (Podophyllotoxin)
[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:171223
[St] Status:MEDLINE


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[PMID]:28696028
[Au] Autor:Ozuah NW; Dahmoush HM; Grant FD; Lehmann LE; LaCasce AS; Billett AL; Margossian SP
[Ad] Endereço:Department of Pediatric Hematology/Oncology, Dana-Farber/Boston Children's Cancer and Blood Disorders Center, Harvard Medical School, Boston, Massachusetts.
[Ti] Título:Pretransplant functional imaging and outcome in pediatric patients with relapsed/refractory Hodgkin lymphoma undergoing autologous transplantation.
[So] Source:Pediatr Blood Cancer;65(1), 2018 Jan.
[Is] ISSN:1545-5017
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Pretransplant functional imaging (FI), particularly a negative positron emission tomography (PET), is a strong predictor of outcome in adults with relapsed or refractory Hodgkin lymphoma (HL), but data in pediatrics are limited. METHODS: The medical records of 49 consecutive pediatric patients, who received autologous transplant at a single institution, were retrospectively analyzed. All patients had either gallium or PET scan before transplant and were conditioned with carmustine, etoposide, cytarabine, and melphalan (BEAM). Deauville scores were retrospectively assigned for patients with PET (score ≥ 4 positive). RESULTS: Of the 49 patients (median age, 16.2 years), 41 (84%) were pretransplant FI negative and eight (16%) were pretransplant FI positive, after first- to fourth-line salvage therapy, and a median of two salvage cycles. Eighteen patients (37%) received posttransplant radiation. At a median follow up of 46 months, 45 patients (92%) were alive and disease free, and there were three nonrelapse deaths and only one relapse death (Deauville score of 5). The 4-year progression-free survival (PFS) for the entire cohort was 92% (95% confidence interval [CI]: 78-97), and PFS based on pretransplant disease status was 95% (95% CI: 82-99%) in the negative FI group versus 75% (95% CI: 31-93) if positive FI (P = 0.057). CONCLUSION: Our analysis revealed outstanding outcomes for children and adolescents with relapsed/refractory HL. There were too few relapses to identify the predictive value of pretransplant metabolic status, but pediatric patients with relapsed/refractory HL and a negative pretransplant FI had excellent survival.
[Mh] Termos MeSH primário: Protocolos de Quimioterapia Combinada Antineoplásica/administração & dosagem
Doença de Hodgkin
Tomografia por Emissão de Pósitrons
Cuidados Pré-Operatórios
Transplante de Células-Tronco
[Mh] Termos MeSH secundário: Adolescente
Adulto
Autoenxertos
Carmustina/administração & dosagem
Criança
Citarabina/administração & dosagem
Intervalo Livre de Doença
Feminino
Seguimentos
Doença de Hodgkin/diagnóstico por imagem
Doença de Hodgkin/mortalidade
Doença de Hodgkin/terapia
Seres Humanos
Masculino
Melfalan/administração & dosagem
Podofilotoxina/administração & dosagem
Estudos Retrospectivos
Taxa de Sobrevida
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE
[Nm] Nome de substância:
04079A1RDZ (Cytarabine); L36H50F353 (Podophyllotoxin); Q41OR9510P (Melphalan); U68WG3173Y (Carmustine)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171201
[Lr] Data última revisão:
171201
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170712
[St] Status:MEDLINE
[do] DOI:10.1002/pbc.26707


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[PMID]:28977631
[Au] Autor:Wang YR; Chen SF; Wu CC; Liao YW; Lin TS; Liu KT; Chen YS; Li TK; Chien TC; Chan NL
[Ad] Endereço:Institute of Biochemistry and Molecular Biology, College of Medicine, National Taiwan University, Taipei 100, Taiwan.
[Ti] Título:Producing irreversible topoisomerase II-mediated DNA breaks by site-specific Pt(II)-methionine coordination chemistry.
[So] Source:Nucleic Acids Res;45(18):10861-10871, 2017 Oct 13.
[Is] ISSN:1362-4962
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Human type II topoisomerase (Top2) isoforms, hTop2α and hTop2ß, are targeted by some of the most successful anticancer drugs. These drugs induce Top2-mediated DNA cleavage to trigger cell-death pathways. The potency of these drugs correlates positively with their efficacy in stabilizing the enzyme-mediated DNA breaks. Structural analysis of hTop2α and hTop2ß revealed the presence of methionine residues in the drug-binding pocket, we therefore tested whether a tighter Top2-drug association may be accomplished by introducing a methionine-reactive Pt2+ into a drug to further stabilize the DNA break. Herein, we synthesized an organoplatinum compound, etoplatin-N2ß, by replacing the methionine-juxtaposing group of the drug etoposide with a cis-dichlorodiammineplatinum(II) moiety. Compared to etoposide, etoplatin-N2ß more potently inhibits both human Top2s. While the DNA breaks arrested by etoposide can be rejoined, those captured by etoplatin-N2ß are practically irreversible. Crystallographic analyses of hTop2ß complexed with DNA and etoplatin-N2ß demonstrate coordinate bond formation between Pt2+ and a flanking methionine. Notably, this stable coordinate tether can be loosened by disrupting the structural integrity of drug-binding pocket, suggesting that Pt2+ coordination chemistry may allow for the development of potent inhibitors with protein conformation-dependent reversibility. This approach may be exploited to achieve isoform-specific targeting of human Top2s.
[Mh] Termos MeSH primário: Antineoplásicos/química
Quebras de DNA
Proteínas de Ligação a DNA/antagonistas & inibidores
Compostos Organoplatínicos/química
Podofilotoxina/análogos & derivados
Inibidores da Topoisomerase II/química
[Mh] Termos MeSH secundário: Antígenos de Neoplasias/química
Antineoplásicos/farmacologia
Linhagem Celular Tumoral
DNA/química
DNA Topoisomerases Tipo II/química
Proteínas de Ligação a DNA/química
Células HL-60
Seres Humanos
Metionina/química
Compostos Organoplatínicos/farmacologia
Podofilotoxina/química
Podofilotoxina/farmacologia
Proteínas de Ligação a Poli-ADP-Ribose
Conformação Proteica
Inibidores da Topoisomerase II/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antigens, Neoplasm); 0 (Antineoplastic Agents); 0 (DNA-Binding Proteins); 0 (Organoplatinum Compounds); 0 (Poly-ADP-Ribose Binding Proteins); 0 (Topoisomerase II Inhibitors); 0 (etoplatin-N2beta); 9007-49-2 (DNA); AE28F7PNPL (Methionine); EC 5.99.1.3 (DNA Topoisomerases, Type II); EC 5.99.1.3 (TOP2A protein, human); L36H50F353 (Podophyllotoxin)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171005
[St] Status:MEDLINE
[do] DOI:10.1093/nar/gkx742


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[PMID]:28972999
[Au] Autor:Mohammed RH; Anderton H; Brameld JM; Sweetman D
[Ad] Endereço:School of Biosciences, University of Nottingham, Sutton Bonington Campus, Loughborough, United Kingdom.
[Ti] Título:Effects of insulin like growth factors on early embryonic chick limb myogenesis.
[So] Source:PLoS One;12(10):e0185775, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Limb muscles derive from pax3 expressing precursor cells that migrate from the hypaxial somite into the developing limb bud. Once there they begin to differentiate and express muscle determination genes such as MyoD. This process is regulated by a combination of inductive or inhibitory signals including Fgf18, retinoic acid, HGF, Notch and IGFs. IGFs are well known to affect late stages of muscle development and to promote both proliferation and differentiation. We examined their roles in early stage limb bud myogenesis using chicken embryos as an experimental model. Grafting beads soaked in purified recombinant IGF-I, IGF-II or small molecule inhibitors of specific signaling pathways into developing chick embryo limbs showed that both IGF-I and IGF-II induce expression of the early stage myogenic markers pax3 and MyoD as well as myogenin. Their effects on pax3 and MyoD expression were blocked by inhibitors of both the IGF type I receptor (picropodophyllotoxin, PPP) and MEK (U0126). The PI3K inhibitor LY294002 blocked IGF-II, but not IGF-I, induction of pax3 mRNA as well as the IGF-I, but not IGF-II, induction of MyoD mRNA. In addition SU5402, an FGFR/ VEGFR inhibitor, blocked the induction of MyoD by both IGFs but had no effect on pax3 induction, suggesting a role for FGF or VEGF signaling in their induction of MyoD. This was confirmed by in situ hybridization showing that FGF18, a known regulator of MyoD in limb myoblasts, was induced by IGF-I. In addition to their well-known effects on later stages of myogenesis via their induction of myogenin expression, both IGF-I and IGF-II induced pax3 and MyoD expression in developing chick embryos, indicating that they also regulate early stages of myogenesis. The data suggests that the IGFs may have slightly different effects on IGF1R signal transduction via PI3K and that their stimulatory effects on MyoD expression may be indirect, possibly via induction of FGF18 expression.
[Mh] Termos MeSH primário: Embrião de Galinha/efeitos dos fármacos
Membro Posterior/efeitos dos fármacos
Fator de Crescimento Insulin-Like II/farmacologia
Fator de Crescimento Insulin-Like I/farmacologia
Desenvolvimento Muscular/efeitos dos fármacos
Músculo Esquelético/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Butadienos/farmacologia
Embrião de Galinha/metabolismo
Cromonas/farmacologia
Inibidores Enzimáticos/farmacologia
Fatores de Crescimento de Fibroblastos/genética
Fatores de Crescimento de Fibroblastos/metabolismo
Regulação da Expressão Gênica no Desenvolvimento
Membro Posterior/metabolismo
Morfolinas/farmacologia
Desenvolvimento Muscular/fisiologia
Músculo Esquelético/metabolismo
Proteína MyoD/genética
Proteína MyoD/metabolismo
Miogenina/genética
Miogenina/metabolismo
Nitrilos/farmacologia
Fator de Transcrição PAX3/genética
Fator de Transcrição PAX3/metabolismo
Fosfatidilinositol 3-Quinases/antagonistas & inibidores
Podofilotoxina/análogos & derivados
Podofilotoxina/farmacologia
Pirróis/farmacologia
Receptor IGF Tipo 1/antagonistas & inibidores
Receptores de Fatores de Crescimento do Endotélio Vascular/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Butadienes); 0 (Chromones); 0 (Enzyme Inhibitors); 0 (Morpholines); 0 (MyoD Protein); 0 (Myogenin); 0 (Nitriles); 0 (PAX3 Transcription Factor); 0 (Pyrroles); 0 (SU 5402); 0 (U 0126); 0 (fibroblast growth factor 18); 0F35AOI227 (picropodophyllin); 31M2U1DVID (2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one); 62031-54-3 (Fibroblast Growth Factors); 67763-96-6 (Insulin-Like Growth Factor I); 67763-97-7 (Insulin-Like Growth Factor II); EC 2.7.1.- (Phosphatidylinositol 3-Kinases); EC 2.7.10.1 (Receptor, IGF Type 1); EC 2.7.10.1 (Receptors, Vascular Endothelial Growth Factor); L36H50F353 (Podophyllotoxin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171004
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0185775


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[PMID]:28879595
[Au] Autor:Partanen A; Valtola J; Ropponen A; Vasala K; Penttilä K; Ågren L; Pyörälä M; Nousiainen T; Selander T; Mäntymaa P; Pelkonen J; Varmavuo V; Jantunen E
[Ad] Endereço:Department of Medicine, Kuopio University Hospital, P.O.B. 100, 70029 KYS, Kuopio, Finland. anu.partanen@kuh.fi.
[Ti] Título:Preemptive plerixafor injection added to pegfilgrastim after chemotherapy in non-Hodgkin lymphoma patients mobilizing poorly.
[So] Source:Ann Hematol;96(11):1897-1906, 2017 Nov.
[Is] ISSN:1432-0584
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Filgrastim is usually combined with chemotherapy to mobilize hematopoietic progenitor cells in non-Hodgkin lymphoma (NHL) patients. Limited information is available on the efficacy of a preemptive plerixafor (PLER) injection in poor mobilizers after chemotherapy and pegfilgrastim. In this prospective study, 72 patients with NHL received chemotherapy plus pegfilgrastim, and 25 hard-to-mobilize patients received also PLER. The usefulness and efficacy of our previously developed algorithm for PLER use in pegfilgrastim-containing mobilization regimen were evaluated as well as the graft cellular composition, hematological recovery, and outcome after autologous stem cell transplantation (auto-SCT) according to the PLER use. A median 3.4-fold increase in blood CD34 cell counts was achieved after the first PLER dose. The minimum collection target was achieved in the first mobilization attempt in 66/72 patients (92%) and 68 patients (94%) proceeded to auto-SCT. An algorithm for PLER use was fulfilled in 76% of the poor mobilizers. Absolute numbers of T-lymphocytes and NK cells were significantly higher in the PLER group, whereas the number of CD34 cells collected was significantly lower. Early neutrophil engraftment was slower in the PLER group, otherwise hematological recovery was comparable within 12 months from auto-SCT. No difference was observed in survival according to the PLER use. Chemotherapy plus pegfilgrastim combined with preemptive PLER injection is an effective and convenient approach to minimize collection failures in NHL patients intended for auto-SCT. A significant effect of PLER on the graft cellular composition was observed, but no difference in outcome after auto-SCT was detected.
[Mh] Termos MeSH primário: Protocolos de Quimioterapia Combinada Antineoplásica/administração & dosagem
Fator Estimulador de Colônias de Granulócitos/administração & dosagem
Mobilização de Células-Tronco Hematopoéticas/tendências
Compostos Heterocíclicos/administração & dosagem
Linfoma não Hodgkin/terapia
[Mh] Termos MeSH secundário: Adulto
Idoso
Carmustina/administração & dosagem
Citarabina/administração & dosagem
Quimioterapia Combinada
Feminino
Filgrastim
Mobilização de Células-Tronco Hematopoéticas/métodos
Seres Humanos
Injeções Subcutâneas
Linfoma não Hodgkin/sangue
Linfoma não Hodgkin/diagnóstico
Masculino
Melfalan/administração & dosagem
Meia-Idade
Podofilotoxina/administração & dosagem
Polietilenoglicóis
Estudos Prospectivos
Proteínas Recombinantes/administração & dosagem
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Heterocyclic Compounds); 0 (Recombinant Proteins); 04079A1RDZ (Cytarabine); 143011-72-7 (Granulocyte Colony-Stimulating Factor); 155148-31-5 (JM 3100); 30IQX730WE (Polyethylene Glycols); 3A58010674 (pegfilgrastim); L36H50F353 (Podophyllotoxin); PVI5M0M1GW (Filgrastim); Q41OR9510P (Melphalan); U68WG3173Y (Carmustine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170908
[St] Status:MEDLINE
[do] DOI:10.1007/s00277-017-3123-6


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[PMID]:28864414
[Au] Autor:Niu L; Wang Y; Wang C; Wang Y; Jiang X; Ma L; Wu C; Yu Y; Chen Q
[Ad] Endereço:Cancer Center, West China Hospital, Sichuan University, Collaborative Innovation Center of Biotherapy, Chengdu, 610041, PR China.
[Ti] Título:Structure of 4'-demethylepipodophyllotoxin in complex with tubulin provides a rationale for drug design.
[So] Source:Biochem Biophys Res Commun;493(1):718-722, 2017 Nov 04.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Microtubules consists of αß-tubulin heterodimers and are highly attractive targets for anti-cancer drugs. A broad range of agents have been identified to bind to tubulin and interfere with microtubule assembly, including colchicine binding site inhibitors (CBSIs). Podophyllotoxin is a CBSI that inhibits the assembly of microtubules. However, for a long time, the design and development of podophyllotoxin family drugs have been hindered by the lack of high-resolution structural information of the tubulin-agent complex. We report the first high-resolution (2.8 Å) structure of a podophyllotoxin family agent (4'-demethylepipodophyllotoxin, DMEP) complexed with tubulin and revealed the detailed interactions between DMEP and tubulin. Comparison of this structure and other CBSIs explains previous results of the structure-activity-relationship (SAR) studies, and provides insights into the development of new podophyllotoxin derivatives targeting the colchicine site.
[Mh] Termos MeSH primário: Desenho de Drogas
Simulação de Acoplamento Molecular
Podofilotoxina/análogos & derivados
Moduladores de Tubulina/química
Tubulina (Proteína)/química
Tubulina (Proteína)/ultraestrutura
[Mh] Termos MeSH secundário: Sítios de Ligação
Podofilotoxina/química
Ligação Proteica
Conformação Proteica
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Tubulin); 0 (Tubulin Modulators); L36H50F353 (Podophyllotoxin); X0S6I23X6L (4'-demethylepipodophyllotoxin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170903
[St] Status:MEDLINE


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[PMID]:28757065
[Au] Autor:Sun WX; Ji YJ; Wan Y; Han HW; Lin HY; Lu GH; Qi JL; Wang XM; Yang YH
[Ad] Endereço:State Key Laboratory of Pharmaceutical Biotechnology, NJU-NJFU Joint Institute of Plant Molecular Biology, Nanjing University, Nanjing 210023, China; Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University, Nanjing 210037, China.
[Ti] Título:Design and synthesis of piperazine acetate podophyllotoxin ester derivatives targeting tubulin depolymerization as new anticancer agents.
[So] Source:Bioorg Med Chem Lett;27(17):4066-4074, 2017 09 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In this paper, a series of podophyllotoxin piperazine acetate ester derivatives were synthesized and investigated due to their antiproliferation activity on different human cancer cell lines. Among the congeners, C5 manifested prominent cytotoxicity towards the cancer cells, without causing damage on the non-cancer cells through inhibiting tubulin assembly and having high selectively causing damage on the human breast (MCF-7) cell line (IC =2.78±0.15µM). Treatments of MCF-7 cells with C5 resulted in cell cycle arrest in G2/M phase and microtubule network disruption. Moreover, regarding the expression of cell cycle relative proteins CDK1, a protein required for mitotic initiation was up-regulated. Besides, Cyclin A, Cyclin B1 and Cyclin D1 proteins were down-regulated. Meanwhile, it seems that the effect of C5 on MCF-7 cells apoptosis inducing was observed to be not obvious enough. In addition, docking analysis demonstrated that the congeners occupy the colchicine binding pocket of tubulin.
[Mh] Termos MeSH primário: Acetatos/farmacologia
Antineoplásicos/farmacologia
Desenho de Drogas
Ésteres/farmacologia
Piperazinas/farmacologia
Podofilotoxina/farmacologia
Tubulina (Proteína)/metabolismo
[Mh] Termos MeSH secundário: Acetatos/síntese química
Acetatos/química
Antineoplásicos/síntese química
Antineoplásicos/química
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Ésteres/síntese química
Ésteres/química
Seres Humanos
Células MCF-7
Estrutura Molecular
Piperazinas/síntese química
Piperazinas/química
Podofilotoxina/síntese química
Podofilotoxina/química
Polimerização/efeitos dos fármacos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Acetates); 0 (Antineoplastic Agents); 0 (Esters); 0 (Piperazines); 0 (Tubulin); 1RTM4PAL0V (piperazine); L36H50F353 (Podophyllotoxin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170801
[St] Status:MEDLINE


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[PMID]:28573235
[Au] Autor:Nieto-Yañez OJ; Resendiz-Albor AA; Ruiz-Hurtado PA; Rivera-Yañez N; Rodriguez-Canales M; Rodriguez-Sosa M; Juarez-Avelar I; Rodriguez-Lopez MG; Canales-Martinez MM; Rodriguez-Monroy MA
[Ad] Endereço:Laboratorio de Inmunidad de Mucosas. Sección de Estudios de Posgrado e Investigación. Escuela Superior de Medicina, del Instituto Politécnico Nacional. Av. Plan de San Luis S/N, Colonia Casco de Santo Tomas, Miguel Hidalgo, CP. 11350. Ciudad de México, D.F.
[Ti] Título: AND ANTILEISHMANIAL EFFECTS OF METHANOLIC EXTRACT FROM BARK OF APTERA.
[So] Source:Afr J Tradit Complement Altern Med;14(2):188-197, 2017.
[Is] ISSN:2505-0044
[Cp] País de publicação:Nigeria
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Cutaneous leishmaniasis lacks effective and well-tolerated treatments. The current therapies mainly rely on antimonial drugs that are inadequate because of their poor efficacy. Traditional medicine offers a complementary alternative for the treatment of various diseases. Additionally, several plants have shown success as anti-leishmanial agents. Therefore, we sought to evaluate the and activity of MEBA against . MATERIALS AND METHODS: Methanolic extract of was obtained by macetration, after we determined anti-leishmanial activity of MEBA by MTT assay and the induced apoptosis in promastigotes by flow cytometry. To analyze the anti-leishmanial activity, we used infected mice that were treated and not treated with MEBA and we determined the levels of cytokines using ELISA. The phytochemical properties were determined by CG-MS and DPPH assay. RESULTS: We determined of LC of 0.408 mg/mL of MEBA for anti-leishmanial activity. MEBA induced apoptosis in promastigotes (15.3% ± 0.86). Treated mice exhibited smaller lesions and contained significantly fewer parasites than did untreated mice; in addition, we found that IFN-γ and TNF-α increased in the sera of MEBA-treated mice. GC-MS analysis showed that podophyllotoxin was the most abundant compound. Evaluation of the activity by DPPH assay demonstrated an SC of 11.72 µg/mL. CONCLUSION: Based on the above data, it was concluded that MEBA is a good candidate in the search for new anti-leishmanial agents.
[Mh] Termos MeSH primário: Bursera/química
Leishmania mexicana
Leishmaniose Cutânea/tratamento farmacológico
Fitoterapia
Extratos Vegetais/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Feminino
Interferon gama/sangue
Leishmaniose Cutânea/sangue
Leishmaniose Cutânea/parasitologia
Medicina Tradicional
Camundongos Endogâmicos BALB C
Casca de Planta
Extratos Vegetais/farmacologia
Podofilotoxina/análise
Podofilotoxina/farmacologia
Podofilotoxina/uso terapêutico
Fator de Necrose Tumoral alfa/sangue
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Plant Extracts); 0 (Tumor Necrosis Factor-alpha); 82115-62-6 (Interferon-gamma); L36H50F353 (Podophyllotoxin)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170816
[Lr] Data última revisão:
170816
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170603
[St] Status:MEDLINE
[do] DOI:10.21010/ajtcam.v14i2.20



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