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[PMID]:28139012
[Au] Autor:Caporale A; Doti N; Sandomenico A; Ruvo M
[Ad] Endereço:IBB-CNR and CIRPeB, Via Mezzocannone 16, 80134, Naples, Italy.
[Ti] Título:Evaluation of combined use of Oxyma and HATU in aggregating peptide sequences.
[So] Source:J Pept Sci;23(4):272-281, 2017 Apr.
[Is] ISSN:1099-1387
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Polypeptides are finding increasing applications as therapeutics because of their specificity that often translates into excellent safety, tolerability, and efficacy profiles in humans. New synthetic methodologies for their preparation are thereby continuously sought to reduce the costs associated to chain assembly and purification. Although solid-phase peptide synthesis has become one of the most advanced synthetic procedures at both laboratory and industrial scale, the process is often complicated by aggregation phenomena originating from the combined occurrence of intermolecular and intramolecular hydrogen bonding, hydrophobic interactions, or other effects. Altogether, these effects cause accumulation of many side products and synthetic mixtures extremely hard to separate and purify, strongly affecting the costs of the final material. In the attempt to optimize the coupling steps of some well-known aggregating or otherwise difficult to obtain peptides, we have comparatively investigated the use of Oxyma/DIC and HATU/Sym-collidine as second coupling reagents in double coupling settings for the preparation of some model peptides. Comparative analytical data obtained on the unpurified products with the two different protocols clearly show that the use of Oxyma/DIC largely improves the content of the target molecules in the final crude materials, making the synthesis more convenient and cost-effective. Copyright © 2017 European Peptide Society and John Wiley & Sons, Ltd.
[Mh] Termos MeSH primário: Compostos Aza/química
Peptídeos/síntese química
Pregnadienos/química
Triazóis/química
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Seres Humanos
Peptídeos/química
Técnicas de Síntese em Fase Sólida
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Aza Compounds); 0 (Peptides); 0 (Pregnadienes); 0 (Triazoles); 57361-81-6 (oxyma); TX8XYH09H0 (1-hydroxy-7-azabenzotriazole)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170508
[Lr] Data última revisão:
170508
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170201
[St] Status:MEDLINE
[do] DOI:10.1002/psc.2977


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[PMID]:27030511
[Au] Autor:Musyoka TM; Kanzi AM; Lobb KA; Tastan Bishop Ö
[Ad] Endereço:Research Unit in Bioinformatics (RUBi), Department of Biochemistry and Microbiology, Rhodes University, Grahamstown, South Africa.
[Ti] Título:Structure Based Docking and Molecular Dynamic Studies of Plasmodial Cysteine Proteases against a South African Natural Compound and its Analogs.
[So] Source:Sci Rep;6:23690, 2016 Mar 31.
[Is] ISSN:2045-2322
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Identification of potential drug targets as well as development of novel antimalarial chemotherapies with unique mode of actions due to drug resistance by Plasmodium parasites are inevitable. Falcipains (falcipain-2 and falcipain-3) of Plasmodium falciparum, which catalyse the haemoglobin degradation process, are validated drug targets. Previous attempts to develop peptide based drugs against these enzymes have been futile due to the poor pharmacological profiles and susceptibility to degradation by host enzymes. This study aimed to identify potential non-peptide inhibitors against falcipains and their homologs from other Plasmodium species. Structure based virtual docking approach was used to screen a small non-peptidic library of natural compounds from South Africa against 11 proteins. A potential hit, 5α-Pregna-1,20-dien-3-one (5PGA), with inhibitory activity against plasmodial proteases and selectivity on human cathepsins was identified. A 3D similarity search on the ZINC database using 5PGA identified five potential hits based on their docking energies. The key interacting residues of proteins with compounds were identified via molecular dynamics and free binding energy calculations. Overall, this study provides a basis for further chemical design for more effective derivatives of these compounds. Interestingly, as these compounds have cholesterol-like nuclei, they and their derivatives might be well tolerated in humans.
[Mh] Termos MeSH primário: Antimaláricos/química
Cisteína Endopeptidases/química
Plasmodium falciparum/química
Pregnadienos/química
Proteínas de Protozoários/antagonistas & inibidores
[Mh] Termos MeSH secundário: Produtos Biológicos/química
Catepsinas/química
Bases de Dados de Proteínas
Resistência a Medicamentos
Hemoglobinas/química
Seres Humanos
Ligações de Hidrogênio
Simulação de Acoplamento Molecular
Simulação de Dinâmica Molecular
Plasmodium falciparum/enzimologia
Domínios e Motivos de Interação entre Proteínas
Proteólise
Proteínas de Protozoários/química
Bibliotecas de Moléculas Pequenas/química
África do Sul
Relação Estrutura-Atividade
Termodinâmica
[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 (Biological Products); 0 (Hemoglobins); 0 (Pregnadienes); 0 (Protozoan Proteins); 0 (Small Molecule Libraries); EC 3.4.- (Cathepsins); EC 3.4.22.- (Cysteine Endopeptidases); EC 3.4.22.- (falcipain 2); EC 3.4.22.- (falcipain 3)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160401
[St] Status:MEDLINE
[do] DOI:10.1038/srep23690


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[PMID]:26924581
[Au] Autor:Silva-Ortiz AV; Bratoeff E; Ramírez-Apan MT; García-Becerra R; Ordaz-Rosado D; Noyola-Martínez N; Castillo-Bocanegra R; Barrera D
[Ad] Endereço:Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, Mexico, D.F. 04510, Mexico.
[Ti] Título:Synthesis and biological activity of two pregnane derivatives with a triazole or imidazole ring at C-21.
[So] Source:J Steroid Biochem Mol Biol;159:8-18, 2016 May.
[Is] ISSN:1879-1220
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Pregnane derivatives are studied as agents for the treatment of different hormone-dependent diseases. The biological importance of these steroids is based on their potential use against cancer. In this study, we report the synthesis, characterization and biological activity of two pregnane derivatives with a triazole (3ß-hydroxy-21-(1H-1,2,4-triazol-1-yl)pregna-5,16-dien-20-one; T-OH) or imidazole (3ß-hydroxy-21-(1H-imidazol-1-yl)pregna-5,16-dien-20-one; I-OH) moieties at C-21. These derivatives were synthesized from 16-dehydropregnenolone acetate. The activity on cell proliferation of the compounds was measured on three human cancer cells lines: prostate cancer (PC-3), breast cancer (MCF7) and lung cancer (SK-LU-1). The cytotoxic and antiproliferative effects of T-OH and I-OH were assessed by using SBR and XTT methods, respectively. The gene expressions were evaluated by real time PCR. In addition, results were complemented by docking studies and transactivation assays using an expression vector to progesterone and androgen receptor. Results show that the two compounds inhibited the three cell lines proliferation in a dose-dependent manner. Compound I-OH downregulated the gene expression of the cyclins D1 and E1 in PC-3 and MFC7 cells; however, effect upon Ki-67, EAG1, BIM or survivin genes was not observed. Docking studies show poor interaction with the steroid receptors. Nevertheless, the transactivation assays show a weak antagonist effect of I-OH on progesterone receptor but not androgenic or antiandrogenic actions. In conclusion, the synthesized compounds inhibited cell proliferation as well as genes key to cell cycle of PC-3 and MCF7 cell lines. Therefore, these compounds could be considered a good starting point for the development of novel therapeutic alternatives to treat cancer.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Imidazóis/síntese química
Pregnadienos/síntese química
Triazóis/síntese química
[Mh] Termos MeSH secundário: Antineoplásicos/farmacologia
Apoptose
Proliferação Celular/efeitos dos fármacos
Ensaios de Seleção de Medicamentos Antitumorais
Células HeLa
Seres Humanos
Imidazóis/farmacologia
Concentração Inibidora 50
Simulação de Acoplamento Molecular
Pregnadienos/farmacologia
Triazóis/farmacologia
Vitamina D3 24-Hidroxilase/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (3-hydroxy-21-(1H-1,2,4-triazol-1-yl)pregna-5,16-dien-20-one); 0 (3-hydroxy-21-(1H-imidazol-1-yl)pregna-5,16-dien-20-one); 0 (Antineoplastic Agents); 0 (Imidazoles); 0 (Pregnadienes); 0 (Triazoles); EC 1.14.15.16 (CYP24A1 protein, human); EC 1.14.15.16 (Vitamin D3 24-Hydroxylase)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:161126
[Lr] Data última revisão:
161126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160301
[St] Status:MEDLINE


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[PMID]:26531176
[Au] Autor:Burugupalli S; Shah S; van der Peet PL; Arora S; White JM; Williams SJ
[Ad] Endereço:School of Chemistry and Bio21 Molecular Science and Biotechnology Institute, University of Melbourne, Parkville, Victoria, Australia 3010. sjwill@unimelb.edu.au.
[Ti] Título:Investigation of benzoyloximes as benzoylating reagents: benzoyl-Oxyma as a selective benzoylating reagent.
[So] Source:Org Biomol Chem;14(1):97-104, 2016 Jan 07.
[Is] ISSN:1477-0539
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Hydroxybenzotriazole (HOBt) and HOBt-derived reagents have been classified as Class I explosives, with restrictions on their transportation and storage. We explored a range of benzoylated oxime-based reagents as alternatives to benzoyloxybenzotriazole (BBTZ) for the selective benzoylation of carbohydrate polyols. Benzoylated oximes derived from 2-hydroximino-malononitrile, ethyl 2-hydroximino-2-cyanoacetate (Oxyma), and tert-butyl 2-hydroximino-2-cyanoacetate were most effective for benzoylation of a simple primary alcohol, with yields approaching that obtained for BBTZ. When applied to carbohydrate diols, the most effective reagent was identified as benzoyl-Oxyma. Benzoyl-Oxyma is a highly crystalline, readily prepared alternative to BBTZ, useful in the selective benzoylation of carbohydrate polyols.
[Mh] Termos MeSH primário: Oximas/química
Pregnadienos/química
[Mh] Termos MeSH secundário: Indicadores e Reagentes
Modelos Moleculares
Estrutura Molecular
Triazóis/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (1-(benzoyloxy)benzotriazole); 0 (Indicators and Reagents); 0 (Oximes); 0 (Pregnadienes); 0 (Triazoles); 57361-81-6 (oxyma)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:151216
[Lr] Data última revisão:
151216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151105
[St] Status:MEDLINE
[do] DOI:10.1039/c5ob02092a


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[PMID]:26044064
[Au] Autor:Matet A; Daruich A; Beydoun T; Cosnes J; Bourges JL
[Ad] Endereço:Department of Ophthalmology, Hotel-Dieu Hospital, AP-HP, and Sorbonne Paris Cité University, Paris Descartes faculty of medicine, 1 place du parvis Notre-Dame 75004, Paris, France. alexmatet@gmail.com.
[Ti] Título:Systemic adalimumab induces peripheral corneal infiltrates: a case report.
[So] Source:BMC Ophthalmol;15:57, 2015 Jun 06.
[Is] ISSN:1471-2415
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Tumor necrosis factor-alpha inhibitors are widely used agents in the treatment of immune disorders such as rheumatoid arthritis and inflammatory bowel disease. Despite their anti-inflammatory action, paradoxical drug-induced inflammatory events have been occasionally associated with the use of infliximab, etanercept, and in a lesser extent adalimumab. However, eye involvement is uncommon and anterior uveitis is the only reported ocular adverse manifestation. It can be induced by etanercept, but has also been described during adalimumab therapy. We present here the first report of recurrent peripheral corneal infiltrates following subcutaneous injections of adalimumab. CASE PRESENTATION: A 34 year-old Caucasian woman with Crohn's disease presented to the emergency department with bilateral red eyes and discomfort 36 hours after she received her bimonthly dose of subcutaneous adalimumab. Examination revealed bilateral peripheral corneal infiltrates with characteristic features of immune infiltrates. Symptoms and infiltrates regressed after topical corticosteroid therapy, but recurred after each adalimumab injection over the following weeks. CONCLUSION: Paradoxical immune reactions associated with tumor necrosis factor-alpha inhibitors may result either from hypersensitivity mechanisms, or from immune-complex deposition via anti-adalimumab antibodies. Both mechanisms could explain this newly described manifestation. Care should be taken to search for corneal infiltrates in the event of red eye symptoms during adalimumab therapy since they respond to topical corticosteroids and do not necessarily prompt the discontinuation of the immunosuppressive therapy.
[Mh] Termos MeSH primário: Adalimumab/efeitos adversos
Anti-Inflamatórios/efeitos adversos
Doenças da Córnea/induzido quimicamente
[Mh] Termos MeSH secundário: Administração Tópica
Adulto
Doenças da Córnea/diagnóstico
Doenças da Córnea/tratamento farmacológico
Doença de Crohn/tratamento farmacológico
Dexametasona/uso terapêutico
Substituição de Medicamentos
Feminino
Glucocorticoides/uso terapêutico
Seres Humanos
Injeções Subcutâneas
Soluções Oftálmicas
Pregnadienos/uso terapêutico
Recidiva
Fator de Necrose Tumoral alfa/antagonistas & inibidores
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Glucocorticoids); 0 (Ophthalmic Solutions); 0 (Pregnadienes); 0 (TNF protein, human); 0 (Tumor Necrosis Factor-alpha); 7S5I7G3JQL (Dexamethasone); FYS6T7F842 (Adalimumab); O7M2E4264D (rimexolone)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:150608
[Lr] Data última revisão:
150608
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150606
[St] Status:MEDLINE
[do] DOI:10.1186/s12886-015-0047-6


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[PMID]:25822848
[Au] Autor:Benzon HT; Huntoon MA; Rathmell JP
[Ad] Endereço:Department of Anesthesiology, Northwestern University Feinberg School of Medicine, Chicago, Illinois.
[Ti] Título:Improving the safety of epidural steroid injections.
[So] Source:JAMA;313(17):1713-4, 2015 May 05.
[Is] ISSN:1538-3598
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Dor nas Costas/tratamento farmacológico
Injeções Epidurais/métodos
Guias de Prática Clínica como Assunto
Pregnadienos/administração & dosagem
[Mh] Termos MeSH secundário: Comitês Consultivos
Seres Humanos
Injeções Epidurais/efeitos adversos
Injeções Epidurais/normas
Deslocamento do Disco Intervertebral/tratamento farmacológico
Cervicalgia/tratamento farmacológico
Segurança do Paciente
Pregnadienos/química
Estados Unidos
United States Food and Drug Administration
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Pregnadienes)
[Em] Mês de entrada:1505
[Cu] Atualização por classe:161017
[Lr] Data última revisão:
161017
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:150331
[St] Status:MEDLINE
[do] DOI:10.1001/jama.2015.2912


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[PMID]:25666913
[Au] Autor:Garrido M; González-Arenas A; Camacho-Arroyo I; Cabeza M; Alcaraz B; Bratoeff E
[Ad] Endereço:Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, D.F. 04510, Mexico. Electronic address: mariana6618@hotmail.com.
[Ti] Título:Effect of new hybrids based on 5,16-pregnadiene scaffold linked to an anti-inflammatory drug on the growth of a human astrocytoma cell line (U373).
[So] Source:Eur J Med Chem;93:135-41, 2015 Mar 26.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:In spite of the fact that anaplastic astrocytoma is an uncommon disease, very often the pathology of this disease is associated with lethal effects due to the late diagnosis and unspecific treatments. This paper reports the synthesis and the biological effect on the growth of U373 cell line (human anaplastic astrocytoma) of new hybrid compounds based on 5,16-pregnadiene scaffold linked to an anti-inflammatory drug (6a-e). Moreover, we also determined the cell growth effect of five non-steroidal anti-inflammatory drugs (naproxen, ibuprofen, ketoprofen, indomethacin and sulindac) as well as the free steroidal alcohol 5. The results from this study indicated that sulindac as well as compound 5 decreased the number of U373 cells at different concentrations. However, when an anti-inflammatory drug was bound to the steroidal structure (5), the resulting compounds (6a-e) showed an enhanced biological effect with exception of hybrid 6c. Furthermore, derivative 6e (sulindac hybrid) did not allow cell growth during six days of experiment at a concentration of 10 µM. The overall data indicated that these molecules showed an anti-proliferative activity on anaplastic astrocytoma cell line.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/química
Antineoplásicos/síntese química
Proliferação Celular/efeitos dos fármacos
Pregnadienos/síntese química
Sulindaco/química
[Mh] Termos MeSH secundário: Antineoplásicos/química
Antineoplásicos/farmacologia
Técnicas de Cultura de Células
Linhagem Celular Tumoral
Seres Humanos
Estrutura Molecular
Pregnadienos/química
Pregnadienos/farmacologia
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Antineoplastic Agents); 0 (Pregnadienes); 184SNS8VUH (Sulindac)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:150313
[Lr] Data última revisão:
150313
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150211
[St] Status:MEDLINE


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[PMID]:25577430
[Au] Autor:Bleriot A; Couret C; Lebranchu P; Le Meur G; Weber M
[Ad] Endereço:CHU de Nantes, 1, place Alexis-Ricordeau, 44000 Nantes, France. Electronic address: alice.bleriot@gmail.com.
[Ti] Título:[Keratitis due to foreign bodies from a processionary caterpillar nest].
[Ti] Título:Kératite par projection d'un nid de chenilles processionnaires..
[So] Source:J Fr Ophtalmol;38(1):85-6, 2015 Jan.
[Is] ISSN:1773-0597
[Cp] País de publicação:France
[La] Idioma:fre
[Mh] Termos MeSH primário: Corpos Estranhos no Olho/complicações
Agricultura Florestal
Ceratite/etiologia
Mariposas
Doenças Profissionais/etiologia
[Mh] Termos MeSH secundário: Corticosteroides/uso terapêutico
Adulto
Animais
Antibacterianos/uso terapêutico
Atropina/uso terapêutico
Conjuntivite/etiologia
Corpos Estranhos no Olho/tratamento farmacológico
Migração de Corpo Estranho/etiologia
Seres Humanos
Hiperemia/etiologia
Ceratite/tratamento farmacológico
Larva
Masculino
Mariposas/crescimento & desenvolvimento
Doenças Profissionais/tratamento farmacológico
Pregnadienos/uso terapêutico
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenal Cortex Hormones); 0 (Anti-Bacterial Agents); 0 (Pregnadienes); 7C0697DR9I (Atropine); O7M2E4264D (rimexolone)
[Em] Mês de entrada:1509
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150112
[St] Status:MEDLINE


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[PMID]:23498251
[Au] Autor:de Freitas AG; Dazzi RL; Muraro PI; Schmidt V; Hörner M; Giacomelli C
[Ad] Endereço:Universidade Federal de Santa Maria, Departamento de Química, 97105-970 Santa Maria-RS, Brazil.
[Ti] Título:Film/contact loading method improves the encapsulated amount of triazene anticancer compounds in polymeric micelles.
[So] Source:Mater Sci Eng C Mater Biol Appl;33(4):2221-8, 2013 May 01.
[Is] ISSN:1873-0191
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The development of organic solvent-free methods for the encapsulation of hydrophobic molecules is necessary for advances in micelle-mediated drug delivery. In this study we investigated the film/contact approach in which the use of organic solvents is limited to the preparation of a dry film before encapsulation. Unloaded micelles of five structurally related block copolymers were placed in contact with thin homogeneous films of two hydrophobic triazene anticancer compounds (1-(4-amidophenyl)-3-(4-acetylphenyl)triazene (1) and corresponding triazenido complex with triphenylphosphanegold(I) fragment (2)). The micelle surface becomes saturated with the drug, which eventually penetrates as a front into the core. Because the drug interacts with both the shell and the core microenvironments of micelle during the process, the maximum loading capacities were very sensitive to block copolymer micelle composition, ranging from 2.2 to 20.4% (wt./wt. of polymer). We conclude that micelles with poly[2-(diisopropylamino)ethyl methacrylate] (PDPA) cores are the best option for the encapsulation of triazene compounds because i) they are prepared in absence of organic phase; ii) the drug concentration in the particles is high enough for a therapeutic effect and iii) the responsiveness properties of PDPA is appropriate for practical applications in pH-triggered drug release systems.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Micelas
Polímeros/química
Triazenos/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/química
Precipitação Química
Cinética
Nanopartículas/química
Polietilenoglicóis/química
Pregnadienos/química
Solventes/química
Espectrofotometria Ultravioleta
Triazenos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Micelles); 0 (Polymers); 0 (Pregnadienes); 0 (Solvents); 0 (Triazenes); 0 (pregna-1,4-dien-3-on-20-al); 30IQX730WE (Polyethylene Glycols)
[Em] Mês de entrada:1309
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130319
[St] Status:MEDLINE


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[PMID]:23466231
[Au] Autor:Stulov SV; Mankevich OV; Dugin NO; Novikov RA; Timofeev VP; Misharin AY
[Ad] Endereço:Orekhovich Institute of Biomedical Chemistry, RAMS, Moscow, Russia.
[Ti] Título:Pregna-5,17(20)-dien-21-oyl amides affecting sterol and triglyceride biosynthesis in Hep G2 cells.
[So] Source:Bioorg Med Chem Lett;23(7):2014-8, 2013 Apr 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Synthesis of series [17(20)Z]- and [17(20)E]-pregna-5,17(20)-dien-21-oyl amides, containing polar substituents in amide moiety, based on rearrangement of 17α-bromo-21-iodo-3ß-acetoxypregn-5-en-20-one caused by amines, is presented. The titled compounds were evaluated for their potency to regulate sterol and triglyceride biosynthesis in human hepatoma Hep G2 cells in comparison with 25-hydroxycholesterol. Three [17(20)E]-pregna-5,17(20)-dien-21-oyl amides at a concentrations of 5 µM inhibited sterol biosynthesis and stimulated triglyceride biosynthesis; their regulatory potency was dependent on the structure of amide moiety; the isomeric [17(20)Z]-pregna-5,17(20)-dien-21-oyl amides were inactive.
[Mh] Termos MeSH primário: Amidas/farmacologia
Pregnadienos/farmacologia
Esteróis/antagonistas & inibidores
Triglicerídeos/antagonistas & inibidores
[Mh] Termos MeSH secundário: Amidas/síntese química
Amidas/química
Relação Dose-Resposta a Droga
Células Hep G2
Seres Humanos
Conformação Molecular
Pregnadienos/síntese química
Pregnadienos/química
Esteróis/biossíntese
Triglicerídeos/biossíntese
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amides); 0 (Pregnadienes); 0 (Sterols); 0 (Triglycerides)
[Em] Mês de entrada:1309
[Cu] Atualização por classe:130318
[Lr] Data última revisão:
130318
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130308
[St] Status:MEDLINE



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