Base de dados : MEDLINE
Pesquisa : G02.111.053 [Categoria DeCS]
Referências encontradas : 2219 [refinar]
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  1 / 2219 MEDLINE  
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[PMID]:27770415
[Au] Autor:Knezevic-Jugovic ZD; Grbavcic SZ; Jovanovic JR; Stefanovic AB; Bezbradica DI; Mijin DZ; Antov MG
[Ad] Endereço:Department for Biochemical Engineering and Biotechnology, Faculty of Technology and Metallurgy, University of Belgrade, Karnegijeva 4, Belgrade, Serbia. zknez@tmf.bg.ac.rs.
[Ti] Título:Covalent Immobilization of Enzymes on Eupergit Supports: Effect of the Immobilization Protocol.
[So] Source:Methods Mol Biol;1504:75-91, 2017.
[Is] ISSN:1940-6029
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A selection of best combination of adequate immobilization support and efficient immobilization method is still a key requirement for successful application of immobilized enzymes on an industrial level. Eupergit supports exhibit good mechanical and chemical properties and allow establishment of satisfactory hydrodynamic regime in enzyme reactors. This is advantageous for their wide application in enzyme immobilization after finding the most favorable immobilization method. Methods for enzyme immobilization that have been previously reported as efficient considering the obtained activity of immobilized enzyme are presented: direct binding to polymers via their epoxy groups, binding to polymers via a spacer made from ethylene diamine/glutaraldehyde, and coupling the periodate-oxidized sugar moieties of the enzymes to the polymer beads. The modification of the conventionally immobilized enzyme with ethylenediamine via the carbodiimide route seems to be a powerful tool to improve its stability and catalytic activity.
[Mh] Termos MeSH primário: Candida/enzimologia
Enzimas Imobilizadas/química
Compostos de Epóxi/química
Etilenodiaminas/química
Glutaral/química
Lipase/química
Polímeros/química
[Mh] Termos MeSH secundário: Acrilamidas/química
Aminação
Candida/química
Candida/metabolismo
Estabilidade Enzimática
Enzimas Imobilizadas/metabolismo
Lipase/metabolismo
Metacrilatos/química
Oxirredução
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acrylamides); 0 (Enzymes, Immobilized); 0 (Epoxy Compounds); 0 (Ethylenediamines); 0 (Methacrylates); 0 (Polymers); 60V9STC53F (ethylenediamine); 93356-75-3 (Eupergit C); EC 3.1.1.3 (Lipase); K67NG89J77 (methacrylamide); T3C89M417N (Glutaral)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180115
[Lr] Data última revisão:
180115
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161023
[St] Status:MEDLINE


  2 / 2219 MEDLINE  
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[PMID]:27770416
[Au] Autor:Besic S; Minteer SD
[Ad] Endereço:Department of Chemistry, Saint Louis University, Saint Louis, MO, 63103, USA.
[Ti] Título:Micellar Polymer Encapsulation of Enzymes.
[So] Source:Methods Mol Biol;1504:93-108, 2017.
[Is] ISSN:1940-6029
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Although enzymes are highly efficient and selective catalysts, there have been problems incorporating them into fuel cells. Early enzyme-based fuel cells contained enzymes in solution rather than immobilized on the electrode surface. One problem utilizing an enzyme in solution is an issue of transport associated with long diffusion lengths between the site of bioelectrocatalysis and the electrode. This issue drastically decreases the theoretical overall power output due to the poor electron conductivity. On the other hand, enzymes immobilized at the electrode surface have eliminated the issue of poor electron conduction due to close proximity of electron transfer between electrode and the biocatalyst. Another problem is inefficient and short term stability of catalytic activity within the enzyme that is suspended in free flowing solution. Enzymes in solutions are only stable for hours to days, whereas immobilized enzymes can be stable for weeks to months and now even years. Over the last decade, there has been substantial research on immobilizing enzymes at electrode surfaces for biofuel cell and sensor applications. The most commonly used techniques are sandwich or wired. Sandwich techniques are powerful and successful for enzyme immobilization; however, the enzymes optimal activity is not retained due to the physical distress applied by the polymer limiting its applications as well as the non-uniform distribution of the enzyme and the diffusion of analyte through the polymer is slowed significantly. Wired techniques have shown to extend the lifetime of an enzyme at the electrode surface; however, this technique is very hard to master due to specific covalent bonding of enzyme and polymer which changes the three-dimensional configuration of enzyme and with that decreases the optimal catalytic activity. This chapter details encapsulation techniques where an enzyme will be immobilized within the pores/pockets of the hydrophobically modified micellar polymers such as Nafion and chitosan. This strategy has been shown to safely immobilize enzymes at electrode surfaces with storage and continuous operation lifetime of more than 2 years.
[Mh] Termos MeSH primário: Quitosana/análogos & derivados
Enzimas Imobilizadas/química
Polímeros de Fluorcarboneto/química
Micelas
[Mh] Termos MeSH secundário: Aminação
Fontes de Energia Bioelétrica
Técnicas Biossensoriais
Eletrodos
Interações Hidrofóbicas e Hidrofílicas
Oxirredução
Porosidade
Compostos de Amônio Quaternário/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Enzymes, Immobilized); 0 (Fluorocarbon Polymers); 0 (Micelles); 0 (Quaternary Ammonium Compounds); 39464-59-0 (perfluorosulfonic acid); 9012-76-4 (Chitosan)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180115
[Lr] Data última revisão:
180115
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161023
[St] Status:MEDLINE


  3 / 2219 MEDLINE  
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[PMID]:29051364
[Au] Autor:Chen LF; Xu Q
[Ad] Endereço:Research Institute of Electrochemical Energy, National Institute of Advanced Industrial Science and Technology (AIST), Ikeda, Osaka 563-8577, Japan. q.xu@aist.go.jp qxuchem@yzu.edu.cn.
[Ti] Título:Converting MOFs into amination catalysts.
[So] Source:Science;358(6361):304-305, 2017 10 20.
[Is] ISSN:1095-9203
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH secundário: Aminação
Catálise
Estrutura Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; COMMENT
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171103
[Lr] Data última revisão:
171103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171021
[St] Status:MEDLINE
[do] DOI:10.1126/science.aap8004


  4 / 2219 MEDLINE  
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[PMID]:28864149
[Au] Autor:Pianovich NA; Dean M; Lassak A; Reiss K; Jursic BS
[Ad] Endereço:Department of Chemistry, University of New Orleans, New Orleans, LA 70148, USA.
[Ti] Título:Anticancer potential of aminomethylidene-diazinanes I. Synthesis of arylaminomethylidene of diazinetriones and its cytotoxic effects tested in glioblastoma cells.
[So] Source:Bioorg Med Chem;25(19):5068-5076, 2017 Oct 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Diazinane and aryl moieties with vinylamine linkers were synthesized to investigate the importance of their structural variations as potential anti-glioblastoma agents. Structural variations incorporated on to the diazinane moiety included oxa and thio derivatives, each with a variety of nitrogen-bound substituents. The size and shape of the aromatic moiety was varied, with the final variation introducing two carbonyl groups, yielding a substituted anthraquinone. Readily available diazinanes and aryl amines were used asan advantageous foundation. Several parameters were calculated whilst engineering these compounds, including: ClogP, molecular polarizability, polar surface area, minimal molecular projected area, and pK . In addition, a simple and efficient procedure was developed to synthesize these compounds. It was demonstrated that a vinylamine with 1,3-diazinane-2,4,6-trione and 1-anthraquinone moiety is the most promising drug candidate causing almost 70% of LN229 tumor cell death at 1µg/ml. In addition, its molecular polarizability, polar surface area and minimal molecular projected area indicate a possible potential of this molecule for crossing BBB.
[Mh] Termos MeSH primário: Antraquinonas/química
Antraquinonas/farmacologia
Antineoplásicos/química
Antineoplásicos/farmacologia
Barbitúricos/química
Barbitúricos/farmacologia
Glioblastoma/tratamento farmacológico
[Mh] Termos MeSH secundário: Aminação
Antraquinonas/síntese química
Antineoplásicos/síntese química
Barbitúricos/síntese química
Morte Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (5-(((9,10-dioxo-9,10-dihydroanthracen-1-yl)amino)methylidene)-1,3-diazinane-2,4,6-trione); 0 (Anthraquinones); 0 (Antineoplastic Agents); 0 (Barbiturates)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170903
[St] Status:MEDLINE


  5 / 2219 MEDLINE  
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[PMID]:28844141
[Au] Autor:Brand S; Ko EJ; Viayna E; Thompson S; Spinks D; Thomas M; Sandberg L; Francisco AF; Jayawardhana S; Smith VC; Jansen C; De Rycker M; Thomas J; MacLean L; Osuna-Cabello M; Riley J; Scullion P; Stojanovski L; Simeons FRC; Epemolu O; Shishikura Y; Crouch SD; Bakshi TS; Nixon CJ; Reid IH; Hill AP; Underwood TZ; Hindley SJ; Robinson SA; Kelly JM; Fiandor JM; Wyatt PG; Marco M; Miles TJ; Read KD; Gilbert IH
[Ad] Endereço:Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
[Ti] Título:Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.
[So] Source:J Med Chem;60(17):7284-7299, 2017 Sep 14.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Chagas' disease, caused by the protozoan parasite Trypanosoma cruzi, is the most common cause of cardiac-related deaths in endemic regions of Latin America. There is an urgent need for new safer treatments because current standard therapeutic options, benznidazole and nifurtimox, have significant side effects and are only effective in the acute phase of the infection with limited efficacy in the chronic phase. Phenotypic high content screening against the intracellular parasite in infected VERO cells was used to identify a novel hit series of 5-amino-1,2,3-triazole-4-carboxamides (ATC). Optimization of the ATC series gave improvements in potency, aqueous solubility, and metabolic stability, which combined to give significant improvements in oral exposure. Mitigation of a potential Ames and hERG liability ultimately led to two promising compounds, one of which demonstrated significant suppression of parasite burden in a mouse model of Chagas' disease.
[Mh] Termos MeSH primário: Doença de Chagas/tratamento farmacológico
Triazóis/química
Triazóis/uso terapêutico
Tripanossomicidas/química
Tripanossomicidas/uso terapêutico
Trypanosoma cruzi/efeitos dos fármacos
[Mh] Termos MeSH secundário: Aminação
Animais
Cercopithecus aethiops
Doença de Chagas/parasitologia
Descoberta de Drogas
Feminino
Seres Humanos
Camundongos
Relação Estrutura-Atividade
Triazóis/farmacocinética
Triazóis/farmacologia
Tripanossomicidas/farmacocinética
Tripanossomicidas/farmacologia
Células Vero
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Triazoles); 0 (Trypanocidal Agents)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170829
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.7b00463


  6 / 2219 MEDLINE  
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[PMID]:28833946
[Au] Autor:Matzel P; Krautschick L; Höhne M
[Ad] Endereço:Protein Biochemistry, Institute of Biochemistry, University of Greifswald, Felix-Hausdorff-Strasse 4, 17487, Greifswald, Germany.
[Ti] Título:Photometric Characterization of the Reductive Amination Scope of the Imine Reductases from Streptomyces tsukubaensis and Streptomyces ipomoeae.
[So] Source:Chembiochem;18(20):2022-2027, 2017 Oct 18.
[Is] ISSN:1439-7633
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Imine reductases (IREDs) have emerged as promising enzymes for the asymmetric synthesis of secondary and tertiary amines starting from carbonyl substrates. Screening the substrate specificity of the reductive amination reaction is usually performed by time-consuming GC analytics. We found two highly active IREDs in our enzyme collection, IR-20 from Streptomyces tsukubaensis and IR-Sip from Streptomyces ipomoeae, that allowed a comprehensive substrate screening with a photometric NADPH assay. We screened 39 carbonyl substrates combined with 17 amines as nucleophiles. Activity data from 663 combinations provided a clear picture about substrate specificity and capabilities in the reductive amination of these enzymes. Besides aliphatic aldehydes, the IREDs accepted various cyclic (C -C ) and acyclic ketones, preferentially with methylamine. IR-Sip also accepted a range of primary and secondary amines as nucleophiles. In biocatalytic reactions, IR-Sip converted (R)-3-methylcyclohexanone with dimethylamine or pyrrolidine with high diastereoselectivity (>94-96 % de). The nucleophile acceptor spectrum depended on the carbonyl substrate employed. The conversion of well-accepted substrates could also be detected if crude lysates were employed as the enzyme source.
[Mh] Termos MeSH primário: Ensaios Enzimáticos
Iminas/metabolismo
Oxirredutases/metabolismo
Streptomyces/enzimologia
[Mh] Termos MeSH secundário: Aminação
NADP/metabolismo
Fotometria
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Imines); 53-59-8 (NADP); EC 1.- (Oxidoreductases)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170824
[St] Status:MEDLINE
[do] DOI:10.1002/cbic.201700257


  7 / 2219 MEDLINE  
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[PMID]:28753275
[Au] Autor:Sharma R; Kapusetti G; Bhong SY; Roy P; Singh SK; Singh S; Balavigneswaran CK; Mahato KK; Ray B; Maiti P; Misra N
[Ti] Título:Osteoconductive Amine-Functionalized Graphene-Poly(methyl methacrylate) Bone Cement Composite with Controlled Exothermic Polymerization.
[So] Source:Bioconjug Chem;28(9):2254-2265, 2017 Sep 20.
[Is] ISSN:1520-4812
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Bone cement has found extensive usage in joint arthroplasty over the last 50 years; still, the development of bone cement with essential properties such as high fatigue resistance, lower exothermic temperature, and bioactivity has been an unsolved problem. In our present work, we have addressed all of the mentioned shortcomings of bone cement by reinforcing it with graphene (GR), graphene oxide (GO), and surface-modified amino graphene (AG) fillers. These nanocomposites have shown hypsochromic shifts, suggesting strong interactions between the filler material and the polymer matrix. AG-based nanohybrids have shown greater osteointegration and lower cytotoxicity compared to other nanohybrids as well as pristine bone cement. They have also reduced oxidative stress on cells, resulting in calcification within 20 days of the implantation of nanohybrids into the rabbits. They have significantly reduced the exothermic curing temperature to body temperature and increased the setting time to facilitate practitioners, suggesting that reaction temperature and settling time can be dynamically controlled by varying the concentration of the filler. Thermal stability and enhanced mechanical properties have been achieved in nanohybrids vis-à-vis pure bone cement. Thus, this newly developed nanocomposite can create natural bonding with bone tissues for improved bioactivity, longer sustainability, and better strength in the prosthesis.
[Mh] Termos MeSH primário: Cimentos para Ossos/química
Grafite/química
Nanocompostos/química
Polimetil Metacrilato/química
[Mh] Termos MeSH secundário: Aminação
Animais
Substitutos Ósseos/química
Linhagem Celular
Seres Humanos
Teste de Materiais
Nanocompostos/ultraestrutura
Osseointegração
Osteogênese
Polimerização
Coelhos
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bone Cements); 0 (Bone Substitutes); 7782-42-5 (Graphite); 9011-14-7 (Polymethyl Methacrylate)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171009
[Lr] Data última revisão:
171009
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170729
[St] Status:MEDLINE
[do] DOI:10.1021/acs.bioconjchem.7b00241


  8 / 2219 MEDLINE  
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[PMID]:28735760
[Au] Autor:Salman M; St Michael F; Ali A; Jabbar A; Cairns C; Hayes AC; Rahman M; Iqbal M; Haque A; Cox AD
[Ad] Endereço:Vaccine Program, Human Health Therapeutics Portfolio, National Research Council, Ottawa, Canada; Health Biotechnology Division, National Institute for Biotechnology, Faisalabad, Pakistan; Department of Microbiology and Biotechnology, Abasyn University, Peshawar, Pakistan. Electronic address: s.amaza
[Ti] Título:First characterization of immunogenic conjugates of Vi negative Salmonella Typhi O-specific polysaccharides with rEPA protein for vaccine development.
[So] Source:J Immunol Methods;450:27-33, 2017 Nov.
[Is] ISSN:1872-7905
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Efficacious typhoid vaccines for young children will significantly reduce the disease burden in developing world. The Vi polysaccharide based conjugate vaccines (Vi-rEPA) against Salmonella Typhi Vi positive strains has shown high efficacy but may be ineffective against Vi negative S. Typhi. In this study, for the first time, we report the synthesis and evaluation of polysaccharide-protein conjugates of Vi negative S. Typhi as potential vaccine candidates. Four different conjugates were synthesized using recombinant exoprotein A of Pseudomonas aeruginosa (rEPA) and human serum albumin (HSA) as the carrier proteins, using either direct reductive amination or an intermediate linker molecule, adipic acid dihydrazide (ADH). Upon injection into mice, a significantly higher antibody titer was observed in mice administrated with conjugate-1 (OSP-HSA) (P=0.0001) and conjugate 2 (OSP-rEPA) (P≤0.0001) as compared to OSP alone. In contrast, the antibody titer elicited by conjugate 3 (OSP -HSA) and conjugate 4 (OSP -rEPA) were insignificant (P=0.1684 and P=0.3794, respectively). We conclude that reductive amination is the superior method to prepare the S. Typhi OSP glycoconjugate. Moreover, rEPA was a better carrier protein than HSA. Thus OSP-rEPA conjugate seems to be efficacious typhoid vaccines candidate, it may be evaluated further and recommended for the clinical trials.
[Mh] Termos MeSH primário: ADP Ribose Transferases/imunologia
Toxinas Bacterianas/imunologia
Exotoxinas/imunologia
Antígenos O/imunologia
Polissacarídeos Bacterianos/imunologia
Salmonella typhi/imunologia
Vacinas Tíficas-Paratíficas/imunologia
Fatores de Virulência/imunologia
[Mh] Termos MeSH secundário: ADP Ribose Transferases/administração & dosagem
ADP Ribose Transferases/química
Aminação
Animais
Anticorpos Antibacterianos/sangue
Toxinas Bacterianas/administração & dosagem
Toxinas Bacterianas/química
Western Blotting
Eletroforese em Gel de Poliacrilamida
Exotoxinas/administração & dosagem
Exotoxinas/química
Feminino
Imunização
Esquemas de Imunização
Injeções Intraperitoneais
Camundongos Endogâmicos BALB C
Antígenos O/administração & dosagem
Antígenos O/química
Oxirredução
Espectroscopia de Prótons por Ressonância Magnética
Proteínas Recombinantes/imunologia
Albumina Sérica/imunologia
Albumina Sérica Humana
Vacinas Tíficas-Paratíficas/administração & dosagem
Vacinas Tíficas-Paratíficas/química
Vacinas Conjugadas/imunologia
Fatores de Virulência/administração & dosagem
Fatores de Virulência/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ALB protein, human); 0 (Antibodies, Bacterial); 0 (Bacterial Toxins); 0 (Exotoxins); 0 (O Antigens); 0 (Polysaccharides, Bacterial); 0 (Recombinant Proteins); 0 (Serum Albumin); 0 (Typhoid-Paratyphoid Vaccines); 0 (Vaccines, Conjugate); 0 (Virulence Factors); 0 (capsular polysaccharide, Salmonella); EC 2.4.2.- (ADP Ribose Transferases); EC 2.4.2.31 (toxA protein, Pseudomonas aeruginosa); ZIF514RVZR (Serum Albumin, Human)
[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:170725
[St] Status:MEDLINE


  9 / 2219 MEDLINE  
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[PMID]:28612980
[Au] Autor:Wang CS; Wu XF; Dixneuf PH; Soulé JF
[Ad] Endereço:Institut des Sciences Chimiques de Rennes, UMR 6226 CNRS-Université de Rennes, "Organométalliques: Matériaux et Catalyse", Campus de Beaulieu, 35042, Rennes, France.
[Ti] Título:Copper-Catalyzed Oxidative Dehydrogenative C(sp )-H Bond Amination of (Cyclo)Alkanes using NH-Heterocycles as Amine Sources.
[So] Source:ChemSusChem;10(15):3075-3082, 2017 Aug 10.
[Is] ISSN:1864-564X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:A copper-catalyzed oxidative C(sp )-H/N-H coupling of NH-heterocycles with affordable (cyclo)alkanes has been developed. This procedure involves C(sp )-N bond formation through a radical pathway generated by homolytic cleavage of di-tert-butyl peroxide and trapping of the radical(s) by copper catalysts. The reaction tolerates a series of functional groups, such as bromo, fluoro, ester, ketone, nitrile, methyl, and methoxy. free-NH-containing indoles, pyrroles, pyrazoles, indazoles, and benzotriazoles are successfully N-alkylated.
[Mh] Termos MeSH primário: Alcanos/química
Aminas/química
Carbono/química
Cobre/química
Compostos Heterocíclicos/química
Hidrogênio/química
[Mh] Termos MeSH secundário: Aminação
Catálise
Hidrogenação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkanes); 0 (Amines); 0 (Heterocyclic Compounds); 7440-44-0 (Carbon); 789U1901C5 (Copper); 7YNJ3PO35Z (Hydrogen)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170829
[Lr] Data última revisão:
170829
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170615
[St] Status:MEDLINE
[do] DOI:10.1002/cssc.201700783


  10 / 2219 MEDLINE  
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[PMID]:28610978
[Au] Autor:Devambatla RKV; Li W; Zaware N; Choudhary S; Hamel E; Mooberry SL; Gangjee A
[Ad] Endereço:Division of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA 15282, United States.
[Ti] Título:Design, synthesis, and structure-activity relationships of pyrimido[4,5-b]indole-4-amines as microtubule depolymerizing agents that are effective against multidrug resistant cells.
[So] Source:Bioorg Med Chem Lett;27(15):3423-3430, 2017 08 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:To identify the structural features of 9H-pyrimido[4,5-b]indoles as microtubule depolymerizers, pyrimido[4,5-b]indoles 2-8 with varied substituents at the 2-, 4- and 5-positions were designed and synthesized. Nucleophilic displacement of 2,5-substituted-4-chloro-pyrimido[4,5-b]indoles with appropriate arylamines was the final step employed in the synthesis of target compounds 2-8. Compounds 2 and 6 had two-digit nanomolar potency (IC ) against MDA-MB-435, SK-OV-3 and HeLa cancer cells in vitro. Compounds 2 and 6 also depolymerized microtubules comparable to the lead compound 1. Compounds 2, 3, 6 and 8 were effective in cells expressing P-glycoprotein or the ßIII isotype of tubulin, mechanisms that are associated with clinical drug resistance to microtubule targeting drugs. Proton NMR and molecular modeling studies were employed to identify the structural basis for the microtubule depolymerizing activity of pyrimido[4,5-b]indoles.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
Resistência a Medicamentos Antineoplásicos
Indóis/química
Indóis/farmacologia
Moduladores de Tubulina/química
Moduladores de Tubulina/farmacologia
[Mh] Termos MeSH secundário: Aminação
Antineoplásicos/síntese química
Linhagem Celular Tumoral
Resistência a Múltiplos Medicamentos
Seres Humanos
Indóis/síntese química
Microtúbulos/metabolismo
Simulação de Acoplamento Molecular
Neoplasias/tratamento farmacológico
Neoplasias/metabolismo
Pirimidinas/síntese química
Pirimidinas/química
Pirimidinas/farmacologia
Relação Estrutura-Atividade
Tubulina (Proteína)/metabolismo
Moduladores de Tubulina/síntese química
[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 (Antineoplastic Agents); 0 (Indoles); 0 (Pyrimidines); 0 (Tubulin); 0 (Tubulin Modulators)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170615
[St] Status:MEDLINE



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