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Pesquisa : D04.210.500.745.745.379 [Categoria DeCS]
Referências encontradas : 150 [refinar]
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[PMID]:27696769
[Au] Autor:Wu X; You L; Zhang D; Gao M; Li Z; Xu D; Zhang P; Huang L; Zhuang R; Wu H; Zhang X
[Ad] Endereço:Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, Fujian, China.
[Ti] Título:Synthesis and preliminary evaluation of a F-labeled ethisterone derivative [ F]EAEF for progesterone receptor targeting.
[So] Source:Chem Biol Drug Des;89(4):559-565, 2017 Apr.
[Is] ISSN:1747-0285
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:To develop a novel progesterone receptor-targeting probe for positron emission tomography imaging, an ethisterone derivative [ F]EAEF was designed and prepared in high decay-corrected radiochemical yield (30-35%) with good radiochemical purity (>98%). [ F]EAEF is a lipophilic tracer (logP = 0.53 ± 0.06) with very good stability in saline and serum. In the biodistribution study, high radioactivity accumulation of [ F]EAEF were found in uterus (5.73 ± 1.83% ID/g) and ovary (4.05 ± 0.73% ID/g) at 2 hr postinjection (p.i.), which have high progesterone receptor expression after treated with estradiol, while the muscle background has very low uptake (0.50 ± 0.17% ID/g). For positron emission tomography imaging, [ F]EAEF showed high uptake in progesterone receptor-positive MCF-7 tumor (3.15 ± 0.07% ID/g at 2 hr p.i.) with good tumor to muscle ratio (2.90), and obvious lower tumor uptakes were observed in MCF-7 with EAEF blocking (1.84 ± 0.05% ID/g at 2 hr p.i.) or in progesterone receptor-negative MDA-MB-231 tumor (1.80 ± 0.03% ID/g at 2 hr p.i.). Based on the good stability and specificity of [ F]EAEF, it may be a good candidate for imaging progesterone receptor and worth further investigation.
[Mh] Termos MeSH primário: Etisterona/análogos & derivados
Receptores de Progesterona/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Espectroscopia de Ressonância Magnética Nuclear de Carbono-13
Etisterona/farmacocinética
Etisterona/farmacologia
Feminino
Radioisótopos de Flúor/química
Seres Humanos
Células MCF-7
Camundongos
Ovário/metabolismo
Tomografia por Emissão de Pósitrons
Espectroscopia de Prótons por Ressonância Magnética
Espectrometria de Massas em Tandem
Distribuição Tecidual
Útero/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Fluorine Radioisotopes); 0 (Receptors, Progesterone); P201BVY1MJ (Ethisterone)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170704
[Lr] Data última revisão:
170704
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161004
[St] Status:MEDLINE
[do] DOI:10.1111/cbdd.12878


  2 / 150 MEDLINE  
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[PMID]:27488525
[Au] Autor:Wang Y; Dehigaspitiya DC; Levine PM; Profit AA; Haugbro M; Imberg-Kazdan K; Logan SK; Kirshenbaum K; Garabedian MJ
[Ad] Endereço:Department of Urology, New York University School of Medicine, New York, New York.
[Ti] Título:Multivalent Peptoid Conjugates Which Overcome Enzalutamide Resistance in Prostate Cancer Cells.
[So] Source:Cancer Res;76(17):5124-32, 2016 Sep 01.
[Is] ISSN:1538-7445
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Development of resistance to antiandrogens for treating advanced prostate cancer is a growing concern and extends to recently developed therapeutics, including enzalutamide. Therefore, new strategies to block androgen receptor (AR) function in prostate cancer are required. Here, we report the characterization of a multivalent conjugate presenting two bioactive ethisterone ligands arrayed as spatially defined pendant groups on a peptoid oligomer. The conjugate, named Multivalent Peptoid Conjugate 6 (MPC6), suppressed the proliferation of multiple AR-expressing prostate cancer cell lines including those that failed to respond to enzalutamide and ARN509. The structure-activity relationships of MPC6 variants were evaluated, revealing that increased spacing between ethisterone moieties and changes in peptoid topology eliminated its antiproliferative effect, suggesting that both ethisterone ligand presentation and scaffold characteristics contribute to MPC6 activity. Mechanistically, MPC6 blocked AR coactivator-peptide interaction and prevented AR intermolecular interactions. Protease sensitivity assays suggested that the MPC6-bound AR induced a receptor conformation distinct from that of dihydrotestosterone- or enzalutamide-bound AR. Pharmacologic studies revealed that MPC6 was metabolically stable and displayed a low plasma clearance rate. Notably, MPC6 treatment reduced tumor growth and decreased Ki67 and AR expression in mouse xenograft models of enzalutamide-resistant LNCaP-abl cells. Thus, MPC6 represents a new class of compounds with the potential to combat treatment-resistant prostate cancer. Cancer Res; 76(17); 5124-32. ©2016 AACR.
[Mh] Termos MeSH primário: Antagonistas de Androgênios/farmacologia
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Peptoides/farmacologia
Neoplasias da Próstata/patologia
[Mh] Termos MeSH secundário: Antagonistas de Androgênios/química
Animais
Western Blotting
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Etisterona/metabolismo
Seres Humanos
Imuno-Histoquímica
Ligantes
Masculino
Camundongos
Camundongos Endogâmicos NOD
Camundongos SCID
Feniltioidantoína/análogos & derivados
Feniltioidantoína/farmacologia
Reação em Cadeia da Polimerase em Tempo Real
Receptores Androgênicos/metabolismo
Relação Estrutura-Atividade
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (AR protein, human); 0 (Androgen Antagonists); 0 (Ligands); 0 (MDV 3100); 0 (Peptoids); 0 (Receptors, Androgen); 2010-15-3 (Phenylthiohydantoin); P201BVY1MJ (Ethisterone)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170902
[Lr] Data última revisão:
170902
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160805
[St] Status:MEDLINE
[do] DOI:10.1158/0008-5472.CAN-16-0385


  3 / 150 MEDLINE  
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[PMID]:26778492
[Au] Autor:Ma X; Wang Q; Wang L; Huang Y; Liao X; Li H
[Ad] Endereço:College of Chemical Engineering, Sichuan University, Chengdu, 610065, People's Republic of China. lihuilab@sina.com.
[Ti] Título:Investigation on the Interaction of Norgestrel with Human Serum Albumin Using Spectroscopy and Molecular-Docking Method.
[So] Source:J Biochem Mol Toxicol;30(6):287-94, 2016 Jun.
[Is] ISSN:1099-0461
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The interaction of norgestrel with human serum albumin (HSA) was investigated by spectroscopy and molecular-docking methods. Results of spectroscopy methods suggested that the quenching mechanism of norgestrel on HSA was static quenching and that the quenching process was spontaneous. Negative values of thermodynamic parameters (ΔG, ΔH, and ΔS) indicated that hydrogen bonding and van der Waals forces dominated the binding between norgestrel and HSA. Three-dimensional fluorescence spectrum and circular dichroism spectrum showed that the HSA structure was slightly changed by norgestrel. Norgestrel mainly bound with Sudlow site I based on a probe study, as confirmed by molecular-docking results. Competition among similar structures indicated that ethisterone and norethisterone affected the binding of norgestrel with HSA. CH3 in R1 had little effect on norgestrel binding with HSA. The surface hydrophobicity properties of HSA, investigated using 8-anilino-1-naphthalenesulfonic acid, was changed with norgestrel addition.
[Mh] Termos MeSH primário: Anticoncepcionais Orais Sintéticos/química
Etisterona/química
Noretindrona/química
Norgestrel/química
Albumina Sérica/química
[Mh] Termos MeSH secundário: Naftalenossulfonato de Anilina
Sítios de Ligação
Corantes Fluorescentes
Seres Humanos
Ligações de Hidrogênio
Interações Hidrofóbicas e Hidrofílicas
Cinética
Simulação de Acoplamento Molecular
Ligação Proteica
Soluções
Espectrometria de Fluorescência
Termodinâmica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (8-anilino-1-naphthalenesulfonic acid); 0 (Anilino Naphthalenesulfonates); 0 (Contraceptives, Oral, Synthetic); 0 (Fluorescent Dyes); 0 (Serum Albumin); 0 (Solutions); 3J8Q1747Z2 (Norgestrel); P201BVY1MJ (Ethisterone); T18F433X4S (Norethindrone)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170203
[Lr] Data última revisão:
170203
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160119
[St] Status:MEDLINE
[do] DOI:10.1002/jbt.21790


  4 / 150 MEDLINE  
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[PMID]:25580911
[Au] Autor:Guo WJ; Wang YT; Kong DX; Wang JY; Wei QH; Chen GN
[Ad] Endereço:Ministry of Education, Fujian Provincial Key Lab of Analysis and Detection for Food Safety and Institute of Nanomedicine and Nanobiosensing, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108 (P. R. China).
[Ti] Título:Luminescent Ag6Au6 heterometallic ethisterone cluster and probe for estrogen receptor α.
[So] Source:Chemistry;21(11):4205-8, 2015 Mar 09.
[Is] ISSN:1521-3765
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:A heterometallic cluster [Ag6Au6(ethisterone)12] of an unprecedented topology was synthesized and characterized. A sensitive and specific probe for estrogen receptor α (ERα) has been developed for the first time based on the enhancement of the Ag6Au6 luminescence.
[Mh] Termos MeSH primário: Receptor alfa de Estrogênio/metabolismo
Etisterona/metabolismo
[Mh] Termos MeSH secundário: Cobre
Ouro
Seres Humanos
Luminescência
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Estrogen Receptor alpha); 0 (estrogen receptor alpha, human); 7440-57-5 (Gold); 789U1901C5 (Copper); P201BVY1MJ (Ethisterone)
[Em] Mês de entrada:1511
[Cu] Atualização por classe:150302
[Lr] Data última revisão:
150302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150113
[St] Status:MEDLINE
[do] DOI:10.1002/chem.201405925


  5 / 150 MEDLINE  
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[PMID]:25369262
[Au] Autor:Mishra KB; Mishra BB; Tiwari VK
[Ad] Endereço:Department of Chemistry, Centre of Advanced Study, Faculty of Science, Banaras Hindu University, Varanasi 5, India.
[Ti] Título:Efficient synthesis of ethisterone glycoconjugate via bis-triazole linkage.
[So] Source:Carbohydr Res;399:2-7, 2014 Nov 18.
[Is] ISSN:1873-426X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Synthesis of sugar based triazolyl azido-alcohols was accomplished via one pot click reaction of glycosyl alkynes with epichlorohydrin in aqueous medium. All the developed triazolyl azido-alcohols were further utilized for the synthesis of bis-triazolyl ethisterone glycoconjugates using CuAAC reaction. The developed triazole-linked ethisterone glycoconjugates would be crucial in androgen receptor pharmacology and chemical biology.
[Mh] Termos MeSH primário: Etisterona/química
Etisterona/síntese química
Glicoconjugados/química
Glicoconjugados/síntese química
Triazóis/química
[Mh] Termos MeSH secundário: Conformação Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Glycoconjugates); 0 (Triazoles); P201BVY1MJ (Ethisterone)
[Em] Mês de entrada:1509
[Cu] Atualização por classe:141105
[Lr] Data última revisão:
141105
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141105
[St] Status:MEDLINE


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[PMID]:24316164
[Au] Autor:Kumar D; Mishra KB; Mishra BB; Mondal S; Tiwari VK
[Ad] Endereço:Department of Chemistry, Centre of Advanced Study, Faculty of Science, Banaras Hindu University, Varanasi 221005, India.
[Ti] Título:Click chemistry inspired highly facile synthesis of triazolyl ethisterone glycoconjugates.
[So] Source:Steroids;80:71-9, 2014 Feb.
[Is] ISSN:1878-5867
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Numerous deoxy-azido sugars 3 were prepared by the reaction of tosyl/bromo sugars with NaN3 in dry DMF under heating condition. The 1,3-dipolar cycloaddition of deoxy-azido sugars 3 with ethisterone 4 to afford regioselective triazole-linked ethisterone glycoconjugates 5 was investigated in the presence of CuI and DIPEA in dichloromethane or CuSO4·5H2O and sodium ascorbate in aqueous medium. All the developed compounds were characterized by spectroscopic analysis (IR, (1)H &(13)C NMR, and MS spectra). Structure of triazolyl ethisterone glycoconjugate 5a has been further confirmed by its Single Crystal X-ray analysis.
[Mh] Termos MeSH primário: Química Click
Etisterona/análogos & derivados
Glicoconjugados/síntese química
Triazóis/síntese química
[Mh] Termos MeSH secundário: Cristalografia por Raios X
Ciclização
Etisterona/síntese química
Etisterona/química
Glicoconjugados/química
Modelos Moleculares
Conformação Molecular
Triazóis/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Glycoconjugates); 0 (Triazoles); P201BVY1MJ (Ethisterone)
[Em] Mês de entrada:1501
[Cu] Atualização por classe:140120
[Lr] Data última revisão:
140120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131210
[St] Status:MEDLINE


  7 / 150 MEDLINE  
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[PMID]:24068368
[Au] Autor:Lim CE; Ho KK; Cheng NC; Wong FW
[Ad] Endereço:South Western Sydney Clinical School, Faculty of Medicine, University of New South Wales, PO BOX 3256, Blakehurst, New South Wales, Australia, 2221.
[Ti] Título:Combined oestrogen and progesterone for preventing miscarriage.
[So] Source:Cochrane Database Syst Rev;(9):CD009278, 2013 Sep 25.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Historically, oestrogen and progesterone were each commonly used to save threatened pregnancies. In the 1940s it was postulated that their combined use would be synergistic and thereby led to the rationale of combined therapy for women who risked miscarriage. OBJECTIVES: To determine the efficacy and safety of combined oestrogen and progesterone therapy to prevent miscarriage. SEARCH METHODS: We searched the Cochrane Pregnancy and Childbirth Group's Trials Register (23 June 2013) CENTRAL (OVID) (The Cochrane Library 2013, Issue 6 of 12), MEDLINE (OVID) (1946 to June Week 2 2013), OLDMEDLINE (1946 to 1965), Embase (1974 to Week 25 2013), Embase Classic (1947 to 1973), CINAHL (1994 to 23 June 2013) and reference lists of retrieved studies. SELECTION CRITERIA: We included randomised controlled trials that assessed the effectiveness of combined oestrogen and progesterone for preventing miscarriage. We included one stratified randomised trial and one quasi-randomised trials. Cluster-randomised trials were eligible for inclusion but none were identified. We excluded studies published only as abstracts.We included studies that compared oestrogen and progesterone versus placebo or no intervention. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed trials for inclusion and assessed trial quality. Two review authors extracted data. Data were checked for accuracy. MAIN RESULTS: Two trials (281 pregnancies and 282 fetuses) met our inclusion criteria. However, the two trials had significant clinical and methodological heterogeneity such that a meta-analysis combining trial data was considered inappropriate.One trial (involving 161 pregnancies) was based on women with a history of diabetes. It showed no statistically significant difference between using combined oestrogen and progestogen and using placebo for all our proposed primary outcomes, namely, miscarriage (risk ratio (RR) 0.95, 95% confidence interval (CI) 0.32 to 2.80), perinatal death (RR 0.94, 95% CI 0.53 to 1.69) and preterm birth (less than 34 weeks of gestation) (RR 0.91, 95% CI 0.80 to 1.04). In terms of this review's secondary outcomes, use of combined oestrogen and progestogen was associated with an increased risk of maternal cancer in the reproductive system (RR 6.65, 95% CI 1.56 to 28.29). However, for the outcome of cancer other than that of the reproductive system in mothers, there was no difference between groups. Similarly, there were no differences between the combined oestrogen and progestogen group versus placebo for other secondary outcomes reported: low birthweight of less than 2500 g, genital abnormalities in the offspring, abnormalities other than genital tract in the offspring, cancer in the reproductive system in the offspring, or cancer other than of the reproductive system in the offspring.The second study was based on pregnant women who had undergone in-vitro fertilisation (IVF). This study showed no difference in the rate of miscarriage between the combined oestrogen and progesterone group and the no treatment group (RR 0.66, 95% CI 0.23 to 1.85). The study did not report on this review's other primary outcomes (perinatal death or rates of preterm birth), nor on any of our proposed secondary outcomes. AUTHORS' CONCLUSIONS: There is an insufficient evidence from randomised controlled trials to assess the use of combined oestrogen and progesterone for preventing miscarriages. We strongly recommend further research in this area.
[Mh] Termos MeSH primário: Aborto Espontâneo/prevenção & controle
Estrogênios/administração & dosagem
Progesterona/administração & dosagem
[Mh] Termos MeSH secundário: Dietilestilbestrol/administração & dosagem
Combinação de Medicamentos
Etisterona/administração & dosagem
Feminino
Fertilização In Vitro
Seres Humanos
Gravidez
Ensaios Clínicos Controlados Aleatórios como Assunto
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Drug Combinations); 0 (Estrogens); 4G7DS2Q64Y (Progesterone); 731DCA35BT (Diethylstilbestrol); P201BVY1MJ (Ethisterone)
[Em] Mês de entrada:1404
[Cu] Atualização por classe:160602
[Lr] Data última revisão:
160602
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130927
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD009278.pub2


  8 / 150 MEDLINE  
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[PMID]:22871957
[Au] Autor:Levine PM; Lee E; Greenfield A; Bonneau R; Logan SK; Garabedian MJ; Kirshenbaum K
[Ad] Endereço:Department of Chemistry, New York University, New York, New York 10003, United States.
[Ti] Título:Androgen receptor antagonism by divalent ethisterone conjugates in castrate-resistant prostate cancer cells.
[So] Source:ACS Chem Biol;7(10):1693-701, 2012 Oct 19.
[Is] ISSN:1554-8937
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Sustained treatment of prostate cancer with androgen receptor (AR) antagonists can evoke drug resistance, leading to castrate-resistant disease. Elevated activity of the AR is often associated with this highly aggressive disease state. Therefore, new therapeutic regimens that target and modulate AR activity could prove beneficial. We previously introduced a versatile chemical platform to generate competitive and non-competitive multivalent peptoid oligomer conjugates that modulate AR activity. In particular, we identified a linear and a cyclic divalent ethisterone conjugate that exhibit potent anti-proliferative properties in LNCaP-abl cells, a model of castrate-resistant prostate cancer. Here, we characterize the mechanism of action of these compounds utilizing confocal microscopy, time-resolved fluorescence resonance energy transfer, chromatin immunoprecipitation, flow cytometry, and microarray analysis. The linear conjugate competitively blocks AR action by inhibiting DNA binding. In addition, the linear conjugate does not promote AR nuclear localization or co-activator binding. In contrast, the cyclic conjugate promotes AR nuclear localization and induces cell-cycle arrest, despite its inability to compete against endogenous ligand for binding to AR in vitro. Genome-wide expression analysis reveals that gene transcripts are differentially affected by treatment with the linear or cyclic conjugate. Although the divalent ethisterone conjugates share extensive chemical similarities, we illustrate that they can antagonize the AR via distinct mechanisms of action, establishing new therapeutic strategies for potential applications in AR pharmacology.
[Mh] Termos MeSH primário: Antagonistas de Receptores de Andrógenos/farmacologia
Etisterona/análogos & derivados
Etisterona/farmacologia
Neoplasias de Próstata Resistentes à Castração/metabolismo
[Mh] Termos MeSH secundário: Ciclo Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Etisterona/síntese química
Expressão Gênica/efeitos dos fármacos
Células HEK293
Seres Humanos
Masculino
Análise em Microsséries
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Androgen Receptor Antagonists); P201BVY1MJ (Ethisterone)
[Em] Mês de entrada:1507
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120809
[St] Status:MEDLINE
[do] DOI:10.1021/cb300332w


  9 / 150 MEDLINE  
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[PMID]:21334280
[Au] Autor:Ruiz J; Rodríguez V; Cutillas N; Espinosa A; Hannon MJ
[Ad] Endereço:Departamento de Química Inorgánica, Universidad de Murcia, Campus de Espinardo, Murcia, Spain. jruiz@um.es
[Ti] Título:Novel C,N-chelate platinum(II) antitumor complexes bearing a lipophilic ethisterone pendant.
[So] Source:J Inorg Biochem;105(4):525-31, 2011 Apr.
[Is] ISSN:1873-3344
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The novel steroidal carrier ligand 17-α-[4'-ethynyl-dimethylbenzylamine]-17-ß-testosterone (ET-dmba 1) and the steroid--C,N-chelate platinum(II) derivatives [Pt(ET-dmba)Cl(L)] (L = DMSO (2) and PTA (3; PTA =1,3,5-triaza-7-phosphaadamantane)) have been prepared. Values of IC(50) were calculated for the new platinum complexes 2 and 3 against a panel of human tumor cell lines representative of ovarian (A2780 and A2780cisR) and breast cancers (T47D). At 48h incubation time complexes 2 and 3 show very low resistance factors (RF of <2) against an A2780 cell line which has acquired resistant to cisplatin and were more active than cisplatin (about 4-fold for 3) in T47D (AR+, AR=androgen receptor). Compound 1 retains a moderate degree of relative binding affinity (RBA=0.94%) for androgen receptors. The cytotoxicity of the non steroidal platinum analogues [Pt(dmba)Cl(L)] (dmba=dimethylbenzylamine; L=DMSO (4) and PTA (5)) has also been studied for comparison purposes. Theoretical calculations at the BP86/def2-TZVP level of theory on complex 3 have been undertaken.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
Etisterona/análogos & derivados
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Linhagem Celular Tumoral
Etisterona/síntese química
Etisterona/química
Etisterona/farmacologia
Seres Humanos
Modelos Moleculares
Compostos Organoplatínicos/síntese química
Compostos Organoplatínicos/química
Compostos Organoplatínicos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (17-(4'-ethynyldimethylbenzylamine)-17-testosterone); 0 (Antineoplastic Agents); 0 (Organoplatinum Compounds); P201BVY1MJ (Ethisterone)
[Em] Mês de entrada:1108
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110222
[St] Status:MEDLINE
[do] DOI:10.1016/j.jinorgbio.2010.12.005


  10 / 150 MEDLINE  
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[PMID]:20023906
[Au] Autor:Sánchez-Cano C; Hannon MJ
[Ad] Endereço:School of Chemistry, University of Birmingham, Edgbaston, UK B15 2TT.
[Ti] Título:Cytotoxicity, cellular localisation and biomolecular interaction of non-covalent metallo-intercalators with appended sex hormone steroid vectors.
[So] Source:Dalton Trans;(48):10765-73, 2009 Dec 28.
[Is] ISSN:1477-9234
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A range of terpyridine platinum(II) metallo-intercalators with bioactive steroids attached has been created with the aim of localizing cytotoxic drugs. Complexes where the steroid does not interfere with access to the terpyridine are shown to retain potent cytotoxicity and show certain selectivity towards their natural receptors. Because the intercalation of the terpyridine moiety between the bases of the DNA is the origin of the biological activity, a dramatic decrease of the activity is observed when the access to the terpyridine unit is hindered by the steroidal unit.
[Mh] Termos MeSH primário: Antineoplásicos/toxicidade
Etinilestradiol/química
Etisterona/química
Substâncias Intercalantes/toxicidade
Metais/química
Platina/química
[Mh] Termos MeSH secundário: Antineoplásicos/análise
Antineoplásicos/química
Linhagem Celular Tumoral
Dicroísmo Circular
DNA/química
DNA/metabolismo
Seres Humanos
Substâncias Intercalantes/análise
Substâncias Intercalantes/química
Espectrofotometria Ultravioleta
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Intercalating Agents); 0 (Metals); 423D2T571U (Ethinyl Estradiol); 49DFR088MY (Platinum); 9007-49-2 (DNA); P201BVY1MJ (Ethisterone)
[Em] Mês de entrada:1003
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:091222
[St] Status:MEDLINE
[do] DOI:10.1039/b912711a



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