Base de dados : MEDLINE
Pesquisa : D01.132.105 [Categoria DeCS]
Referências encontradas : 1190 [refinar]
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[PMID]:28632381
[Au] Autor:Sárosi MB; Neumann W; Lybrand TP; Hey-Hawkins E
[Ad] Endereço:Institute of Inorganic Chemistry, Faculty of Chemistry and Mineralogy, Leipzig University , Johannisallee 29, D-04103 Leipzig, Germany.
[Ti] Título:Molecular Modeling of the Interactions between Carborane-Containing Analogs of Indomethacin and Cyclooxygenase-2.
[So] Source:J Chem Inf Model;57(8):2056-2067, 2017 Aug 28.
[Is] ISSN:1549-960X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Molecular modeling studies were performed in order to gain insight into the binding mode and interaction of carborane-containing derivatives of indomethacin methyl ester with the cyclooxygenase-2 (COX-2) isoform, and to assess the predictive capability of the computational tools available for studying carboranes, a unique class of pharmacophores. Docking simulations were able to identify the correct binding mode and reproduced the experimental binding affinity trends with encouraging quality. Nevertheless, the docking results needed to be verified through extensive and resource-intensive quantum chemical calculations, and the interpretation of the theoretical results would not have been straightforward without the supporting experimental data. The inclusion of full receptor and ligand flexibility into the molecular modeling of carborane-containing drug molecules may yield more definitive results, but is currently hindered by the lack of appropriate carborane force field parameters.
[Mh] Termos MeSH primário: Boranos/química
Ciclo-Oxigenase 2/metabolismo
Indometacina/química
Indometacina/metabolismo
Simulação de Acoplamento Molecular
[Mh] Termos MeSH secundário: Ciclo-Oxigenase 2/química
Ligantes
Ligação Proteica
Conformação Proteica
Teoria Quântica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Boranes); 0 (Ligands); EC 1.14.99.1 (Cyclooxygenase 2); XXE1CET956 (Indomethacin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170621
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jcim.7b00113


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[PMID]:28351608
[Au] Autor:Ieawsuwan W; Ruchirawat S
[Ad] Endereço:Laboratory of Medicinal Chemistry, Chulabhorn Research Institute, 54 Kamphaeng Phet 6 Road, Laksi, Bangkok 10210, Thailand. Electronic address: winai@cri.or.th.
[Ti] Título:PIFA-BF ·OEt mediated intramolecular regioselective domino cyclization of ynamides: A novel method for the synthesis of tetrahydroisoquinoline-oxazol-2(3H)-ones.
[So] Source:Bioorg Med Chem;25(11):2856-2867, 2017 Jun 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The transition metal-free intramolecular regioselective domino cyclization of N-Boc protected ynamides has been developed to provide the corresponding tetrahydroisoquinoline-oxazo-2(3H)-ones in moderate to good yields.
[Mh] Termos MeSH primário: Acetatos/química
Alquinos/química
Amidas/química
Iodobenzenos/química
Isoquinolinas/síntese química
Oxazóis/síntese química
[Mh] Termos MeSH secundário: Boranos/química
Ciclização
Éter/química
Isoquinolinas/química
Estrutura Molecular
Oxazóis/química
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 ((bis(trifluoroacetoxy)iodo)benzene); 0 (Acetates); 0 (Alkynes); 0 (Amides); 0 (Boranes); 0 (Iodobenzenes); 0 (Isoquinolines); 0 (Oxazoles); 0F5N573A2Y (Ether); 7JGD48PX8P (boron trifluoride)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170718
[Lr] Data última revisão:
170718
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170330
[St] Status:MEDLINE


  3 / 1190 MEDLINE  
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[PMID]:28237752
[Au] Autor:Pant B; Park M; Lee JH; Kim HY; Park SJ
[Ad] Endereço:Department of Chemistry, Inha University, 100 Inharo, Incheon 402-751, Republic of Korea.
[Ti] Título:Novel magnetically separable silver-iron oxide nanoparticles decorated graphitic carbon nitride nano-sheets: A multifunctional photocatalyst via one-step hydrothermal process.
[So] Source:J Colloid Interface Sci;496:343-352, 2017 06 15.
[Is] ISSN:1095-7103
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Development of photocatalytic materials with magnetic and antibacterial properties is highly desirable in wastewater treatment. In this study, a novel magnetically separable silver-iron oxide nanoparticles (Ag-Fe O NPs) decorated graphitic carbon nitride (g-C N ) nanocomposite via hydrothermal treatment has been presented for the multifaceted applications. The physiochemical properties of the as-synthesized ternary nanocomposite were characterized by the field emission scanning electron microscopy (FE-SEM), transmission electron microscopy (TEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), X-ray photoelectron spectroscopy (XPS), and photoluminescence (PL) studies. The experimental results showed that loading of Ag on Fe O /g-C N nanocomposite significantly improved the catalytic activity of the composite material in terms of photocatalytic degradation of methylene blue (Mdestruction of Escherichia coli (E. coli) bacteria. More importantly, the as-synthesized silver-iron oxide nanoparticles decorated graphitic carbon nitride (Ag-Fe O /g-C N ) nanocomposite catalyst could be recovered by an applied external magnet and reused without the loss of photocatalytic activity. The obtained results showed that the synthesized material has potential as an economically friendly photocatalyst for environmental and energy applications.
[Mh] Termos MeSH primário: Antibacterianos/química
Compostos Férricos/química
Grafite/química
Nanopartículas de Magnetita/química
Nitrilos/química
Prata/química
[Mh] Termos MeSH secundário: Antibacterianos/farmacologia
Boranos/química
Boranos/efeitos da radiação
Catálise
Escherichia coli/efeitos dos fármacos
Escherichia coli/efeitos da radiação
Seres Humanos
Hidrólise
Luz
Azul de Metileno/química
Nanocompostos/química
Processos Fotoquímicos
Propriedades de Superfície
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Boranes); 0 (Ferric Compounds); 0 (Magnetite Nanoparticles); 0 (Nitriles); 1K09F3G675 (ferric oxide); 3M4G523W1G (Silver); 534Q0F66RK (cyanogen); 7782-42-5 (Graphite); T42P99266K (Methylene Blue)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171013
[Lr] Data última revisão:
171013
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170227
[St] Status:MEDLINE


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[PMID]:28094467
[Au] Autor:Shahat EA; Bakr RO; Eldahshan OA; Ayoub NA
[Ad] Endereço:Pharmacognosy Department, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Giza, Egypt.
[Ti] Título:Chemical Composition and Biological Activities of the Essential Oil from Leaves and Flowers of Pulicaria incisa sub. candolleana (Family Asteraceae).
[So] Source:Chem Biodivers;14(4), 2017 Apr.
[Is] ISSN:1612-1880
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:The composition of the essential oil isolated from leaves and flowers of Pulicaria incisa sub. candolleana E. Gamal-Eldin, growing in Egypt, was analysed by GC and GC-MS. Forty-nine and 68 compounds were identified from the oils of the leaves and flowers accounting for 86.69 and 84.29%, respectively of the total detected constituents. Both leaves and flowers oils were characterized by the high content of carvotanacetone with 66.01, 50.87 and chrysanthenone 13.26, 24.3%, respectively. The cytotoxic activity of both essential oils was evaluated against hepatocellular carcinoma cell line HEPG-2, using MTT assay and vinblastine as a reference drug. Leaf oil showed higher activity with IC 11.4 µg/ml compared with 37.4 µg/ml for flower oil. The antimicrobial activity of both oils was evaluated using agar well diffusion method towards two representatives for each of Gram positive and Gram negative bacteria as well as four representatives for fungi. The minimum inhibitory concentration of both essential oils against bacterial and fungal strains was obtained in the range of 0.49 - 15.63 µg/ml.
[Mh] Termos MeSH primário: Antibacterianos/isolamento & purificação
Antifúngicos/isolamento & purificação
Antineoplásicos/isolamento & purificação
Óleos Voláteis/química
Pulicaria/química
[Mh] Termos MeSH secundário: Antibacterianos/química
Antifúngicos/química
Antifúngicos/farmacologia
Antineoplásicos/química
Antineoplásicos/farmacologia
Boranos/isolamento & purificação
Egito
Flores/química
Cromatografia Gasosa-Espectrometria de Massas
Bactérias Gram-Negativas/efeitos dos fármacos
Bactérias Gram-Positivas/efeitos dos fármacos
Células Hep G2
Seres Humanos
Testes de Sensibilidade Microbiana
Óleos Voláteis/isolamento & purificação
Óleos Voláteis/farmacologia
Folhas de Planta/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antifungal Agents); 0 (Antineoplastic Agents); 0 (Boranes); 0 (Oils, Volatile); 0 (chrysanthenone)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170424
[Lr] Data última revisão:
170424
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170118
[St] Status:MEDLINE
[do] DOI:10.1002/cbdv.201600156


  5 / 1190 MEDLINE  
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[PMID]:27929169
[Au] Autor:Perrio C; Schmitt S; Pla D; Gabbaï FP; Chansaenpak K; Mestre-Voegtle B; Gras E
[Ad] Endereço:Normandie Univ, UNICAEN, CEA, CNRS, UMR6301-ISTCT, LDM-TEP, Cyceron, Boulevard Henri Becquerel, 14000 Caen, France. perrio@cyceron.fr.
[Ti] Título:[ F]-Fluoride capture and release: azeotropic drying free nucleophilic aromatic radiofluorination assisted by a phosphonium borane.
[So] Source:Chem Commun (Camb);53(2):340-343, 2016 12 22.
[Is] ISSN:1364-548X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:[ F]-Fluoride ready for aromatic nucleophilic substitution was prepared according to a simple process including trapping of aqueous [ F]-fluoride on a cartridge pre-loaded with the phosphonium borane [(Ph MeP)C H (BMes )] , then releasing by elution of TBACN in dry acetonitrile. Subsequent radiofluorination was successfully applied to a model reaction and to the radiosynthesis of [ F]-setoperone.
[Mh] Termos MeSH primário: Boranos/química
Fluoretos/química
Radioisótopos de Flúor/química
Halogenação
Radioquímica/métodos
[Mh] Termos MeSH secundário: Acetonitrilos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Acetonitriles); 0 (Boranes); 0 (Fluorine Radioisotopes); Q80VPU408O (Fluorides); Z072SB282N (acetonitrile)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170726
[Lr] Data última revisão:
170726
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161209
[St] Status:MEDLINE
[do] DOI:10.1039/c6cc05168e


  6 / 1190 MEDLINE  
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[PMID]:27766599
[Au] Autor:Butt U; ElShaer A; Snyder LA; Chaidemenou A; Alany RG
[Ad] Endereço:Drug Discovery, Delivery and Patient Care (DDDPC) Theme, School of Pharmacy and Chemistry, Kingston University London, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, UK.
[Ti] Título:Fatty acid microemulsion for the treatment of neonatal conjunctivitis: quantification, characterisation and evaluation of antimicrobial activity.
[So] Source:Drug Deliv Transl Res;6(6):722-734, 2016 Dec.
[Is] ISSN:2190-3948
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Fatty acids (FAs) are used by many organisms as defence mechanism against virulent bacteria. The high safety profile and broad spectrum of activity make them potential alternatives to currently used topical antibiotics for the treatment of eye infections in neonates. The current study utilised a Design of Experiment approach to optimise the quantification of five fatty acids namely; lauric acid, tridecanoic acid, myristoleic acid, palmitoleic acid and α-linolenic acid. The significance of the influence of the experimental parameters such as volume of catalyst, volume of n-hexane, incubation temperature, incubation time and the number of extraction steps on derivatisation was established by statistical screening with a factorial approach. Derivatisation was confirmed using attenuated total reflectance infrared (ATR) and 1H NMR spectrum. A gas chromatographic method (GC-FID) was developed and validated according to ICH guidelines for the identification and quantification of fatty acids. The results were found to be linear over the concentration range studied with coefficient of variation greater than 0.99 and high recovery values and low intra-day and inter-day variation values for all FAs. Then, different α-linolenic acid-based microemulsions (MEs) were prepared using Tween 80 as surfactant, polyethylene glycol 400 (PEG 400) as co surfactant and water as aqueous phase. The developed GC method was used to quantify the FA content in ME formulations. The results indicated that the developed GC method is very effective to quantify the FA content in the ME formulations. The antimicrobial efficacy of FA-based MEs were tested against Staphylococcus aureus. It was concluded that the FA-based MEs have strong antimicrobial effect against S. aureus.
[Mh] Termos MeSH primário: Antibacterianos/administração & dosagem
Ácidos Graxos/administração & dosagem
Staphylococcus aureus/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antibacterianos/química
Boranos/química
Cloretos/química
Conjuntivite/tratamento farmacológico
Emulsões
Ácidos Graxos/química
Metanol/química
Polietilenoglicóis/química
Polissorbatos/química
Staphylococcus aureus/crescimento & desenvolvimento
Tensoativos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Boranes); 0 (Chlorides); 0 (Emulsions); 0 (Fatty Acids); 0 (Polysorbates); 0 (Surface-Active Agents); 30IQX730WE (Polyethylene Glycols); B697894SGQ (polyethylene glycol 400); K748471RAG (boron trichloride); Y4S76JWI15 (Methanol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171026
[Lr] Data última revisão:
171026
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161106
[St] Status:MEDLINE


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[PMID]:27548011
[Au] Autor:Xiong H; Wei X; Zhou D; Qi Y; Xie Z; Chen X; Jing X; Huang Y
[Ad] Endereço:State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun 130022, PR China.
[Ti] Título:Amphiphilic Polycarbonates from Carborane-Installed Cyclic Carbonates as Potential Agents for Boron Neutron Capture Therapy.
[So] Source:Bioconjug Chem;27(9):2214-23, 2016 Sep 21.
[Is] ISSN:1520-4812
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Carboranes with rich boron content have showed significant applications in the field of boron neutron capture therapy. Biodegradable derivatives of carborane-conjugated polymers with well-defined structure and tunable loading of boron atoms are far less explored. Herein, a new family of amphiphilic carborane-conjugated polycarbonates was synthesized by ring-opening polymerization of a carborane-installed cyclic carbonate monomer. Catalyzed by TBD from a poly(ethylene glycol) macroinitiator, the polymerization proceeded to relatively high conversions (>65%), with low polydispersity in a certain range of molecular weight. The boron content was readily tuned by the feed ratio of the monomer and initiator. The resultant amphiphilic polycarbonates self-assembled in water into spherical nanoparticles of different sizes depending on the hydrophilic-to-hydrophobic ratio. It was demonstrated that larger nanoparticles (PN150) were more easily subjected to protein adsorption and captured by the liver, and smaller nanoparticles (PN50) were more likely to enter cancer cells and accumulate at the tumor site. PN50 with thermal neutron irradiation exhibited the highest therapeutic efficacy in vivo. The new synthetic method utilizing amphiphilic biodegradable boron-enriched polymers is useful for developing more-selective and -effective boron delivery systems for BNCT.
[Mh] Termos MeSH primário: Boranos/química
Terapia por Captura de Nêutron de Boro/métodos
Carbonatos/química
Interações Hidrofóbicas e Hidrofílicas
Cimento de Policarboxilato/química
Cimento de Policarboxilato/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Transporte Biológico
Linhagem Celular Tumoral
Seres Humanos
Camundongos
Nanopartículas/química
Tamanho da Partícula
Cimento de Policarboxilato/metabolismo
Cimento de Policarboxilato/farmacocinética
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Boranes); 0 (Carbonates); 0 (Polycarboxylate Cement); 25766-59-0 (polycarbonate)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170621
[Lr] Data última revisão:
170621
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160823
[St] Status:MEDLINE
[do] DOI:10.1021/acs.bioconjchem.6b00454


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[PMID]:27402268
[Au] Autor:Watanabe K; Hirata M; Tominari T; Matsumoto C; Endo Y; Murphy G; Nagase H; Inada M; Miyaura C
[Ad] Endereço:Department of Biotechnology and Life Science, Tokyo University of Agriculture and Technology, 2-24-16 Nakamachi, Koganei, Tokyo 184-8588, Japan; Cooperative Major in Advanced Health Science, Tokyo University of Agriculture and Technology, 2-24-16 Nakamachi, Koganei, Tokyo 184-8588, Japan.
[Ti] Título:BA321, a novel carborane analog that binds to androgen and estrogen receptors, acts as a new selective androgen receptor modulator of bone in male mice.
[So] Source:Biochem Biophys Res Commun;478(1):279-285, 2016 09 09.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Carboranes are a class of carbon-containing polyhedral boron cluster compounds with globular geometry and hydrophobic surface that interact with hormone receptors such as estrogen receptor (ER) and androgen receptor (AR). We have synthesized BA321, a novel carborane compound, which binds to AR. We found here that it also binds to ERs, ERα and ERß. In orchidectomized (ORX) mice, femoral bone mass was markedly reduced due to androgen deficiency and BA321 restored bone loss in the male, whilst the decreased weight of seminal vesicle in ORX mice was not recovered by administration of BA321. In female mice, BA321 acts as a pure estrogen agonist, and restored both the loss of bone mass and uterine atrophy due to estrogen deficiency in ovariectomized (OVX) mice. In bone tissues, the trabecular bone loss occurred in both ORX and OVX mice, and BA321 completely restored the trabecular bone loss in both sexes. Cortical bone loss occurred in ORX mice but not in OVX mice, and BA321 clearly restored cortical bone loss due to androgen deficiency in ORX mice. Therefore, BA321 is a novel selective androgen receptor modulator (SARM) that may offer a new therapy option for osteoporosis in the male.
[Mh] Termos MeSH primário: Androgênios/metabolismo
Boranos/administração & dosagem
Osteoporose/tratamento farmacológico
Osteoporose/metabolismo
Receptores Androgênicos/metabolismo
Receptores Estrogênicos/metabolismo
[Mh] Termos MeSH secundário: Animais
Osso e Ossos/efeitos dos fármacos
Osso e Ossos/metabolismo
Boranos/farmacocinética
Relação Dose-Resposta a Droga
Feminino
Gônadas/efeitos dos fármacos
Gônadas/metabolismo
Seres Humanos
Masculino
Camundongos
Camundongos Endogâmicos
Orquiectomia
Osteoporose/patologia
Ovariectomia
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Androgens); 0 (Boranes); 0 (Receptors, Androgen); 0 (Receptors, Estrogen)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171127
[Lr] Data última revisão:
171127
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160713
[St] Status:MEDLINE


  9 / 1190 MEDLINE  
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[PMID]:27374514
[Au] Autor:Yurchenko S; Sats A; Poikalainen V; Karus A
[Ad] Endereço:Estonian University of Life Sciences, Institute of Veterinary Medicine and Animal Sciences, Department of Food Science and Technology, Kreutzwaldi 62, EE51014 Tartu, Estonia. Electronic address: sergei.jurtsenko@emu.ee.
[Ti] Título:Method for determination of fatty acids in bovine colostrum using GC-FID.
[So] Source:Food Chem;212:117-22, 2016 Dec 01.
[Is] ISSN:0308-8146
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Bovine colostrum is potentially valuable source of essential fatty acids (FAs), but so far only few studies have made the effort to estimate FA composition of this potential resource. The aim of current research was to fill this gap with selecting and validating an accurate procedure for the analysis of the composition of the FAs in bovine colostrum. We used colostrum samples of Holstein-Friesian cattle from Märja experimental farm as a test material. The validated method includes derivatization, in which FAs are sent through esterification with the acidic catalyst boron trifluoride. Formed methyl esters of fatty acids (FAMEs) were analysed using GC-FID. The obtained LOD and the LOQ of FAMEs were 0.11-0.68 and 0.37-2.27ppm, respectively. The analysis of fortified samples showed very good and similar recoveries, indicating that the method proposed here can be routinely used for determination and investigation of the fatty acids in dairy products.
[Mh] Termos MeSH primário: Cromatografia Gasosa/métodos
Colostro/química
Ácidos Graxos/análise
[Mh] Termos MeSH secundário: Animais
Boranos
Bovinos
Esterificação
Ésteres
Feminino
Gravidez
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Boranes); 0 (Esters); 0 (Fatty Acids); 7JGD48PX8P (boron trifluoride)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170118
[Lr] Data última revisão:
170118
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160705
[St] Status:MEDLINE


  10 / 1190 MEDLINE  
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[PMID]:27371927
[Au] Autor:Kaise A; Ohta K; Endo Y
[Ad] Endereço:Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai, 981-8558, Japan.
[Ti] Título:Design, synthesis, and anti-proliferative activity of 1-(4-methoxyphenyl)-12-hydroxymethyl-p-carborane derivatives.
[So] Source:Eur J Med Chem;122:257-263, 2016 Oct 21.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:1-(4-Methoxyphenyl)-12-hydroxymethyl-p-carborane (2a), which is a precursor to the previously developed potent carborane-containing ER agonist BE120, exhibited weak cell growth inhibitory activity against four human cancer cell lines (MCF-7, MDA-MB-453, LNCaP, and PC-3). The biological evaluation of a series of derivatives of 2a revealed that an increased number of methoxy groups on the benzene ring of 2a enhanced the cell growth inhibitory activity. Trimethoxyphenyl derivative 2g afforded the most potent cell growth inhibitory activity (mean GI50 value: 5.8 µM) in a panel screening using 39 human cancer cell lines. Moreover, 2g induced for MDA-MB-453 breast cancer cell lines an arrest of the cell cycle in the G2/M phase and apoptosis mediated by caspase-3/7.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Antineoplásicos/farmacologia
Boranos/síntese química
Boranos/farmacologia
Desenho de Drogas
[Mh] Termos MeSH secundário: Antineoplásicos/química
Antineoplásicos/metabolismo
Apoptose/efeitos dos fármacos
Ligação Competitiva
Boranos/química
Boranos/metabolismo
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Técnicas de Química Sintética
Ensaios de Seleção de Medicamentos Antitumorais
Receptor alfa de Estrogênio/metabolismo
Seres Humanos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Boranes); 0 (Estrogen Receptor alpha)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170807
[Lr] Data última revisão:
170807
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160703
[St] Status:MEDLINE



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