Base de dados : MEDLINE
Pesquisa : D02.455.426.559.847.638.960.837 [Categoria DeCS]
Referências encontradas : 284 [refinar]
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  1 / 284 MEDLINE  
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[PMID]:28881253
[Au] Autor:Janse van Rensburg HD; Terre'Blanche G; van der Walt MM; Legoabe LJ
[Ad] Endereço:Pharmaceutical Chemistry, School of Pharmacy, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
[Ti] Título:5-Substituted 2-benzylidene-1-tetralone analogues as A and/or A antagonists for the potential treatment of neurological conditions.
[So] Source:Bioorg Chem;74:251-259, 2017 Oct.
[Is] ISSN:1090-2120
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Adenosine A and A receptors are attracting great interest as drug targets for their role in cognitive and motor deficits, respectively. Antagonism of both these adenosine receptors may offer therapeutic benefits in complex neurological diseases, such as Alzheimer's and Parkinson's disease. The aim of this study was to explore the affinity and selectivity of 2-benzylidene-1-tetralone derivatives as adenosine A and A receptor antagonists. Several 5-hydroxy substituted 2-benzylidene-1-tetralone analogues with substituents on ring B were synthesized and assessed as antagonists of the adenosine A and A receptors via radioligand binding assays. The results indicated that hydroxy substitution in the meta and para position of phenyl ring B, displayed the highest selectivity and affinity for the adenosine A receptor with K values in the low micromolar range. Replacement of ring B with a 2-amino-pyrimidine moiety led to compound 12 with an increase of affinity and selectivity for the adenosine A receptor. These substitution patterns led to enhanced adenosine A and A receptor binding affinity. The para-substituted 5-hydroxy analogue 3 behaved as an adenosine A receptor antagonists in a GTP shift assay performed with rat whole brain membranes expressing adenosine A receptors. In conclusion, compounds 3 and 12, showed the best adenosine A and A receptor affinity respectively, and therefore represent novel adenosine receptor antagonists that may have potential with further structural modifications as drug candidates for neurological disorders.
[Mh] Termos MeSH primário: Antagonistas do Receptor A1 de Adenosina/farmacologia
Antagonistas do Receptor A2 de Adenosina/farmacologia
Doenças do Sistema Nervoso/tratamento farmacológico
Receptor A1 de Adenosina/metabolismo
Receptor A2A de Adenosina/metabolismo
Tetralonas/farmacologia
[Mh] Termos MeSH secundário: Antagonistas do Receptor A1 de Adenosina/síntese química
Antagonistas do Receptor A1 de Adenosina/química
Antagonistas do Receptor A2 de Adenosina/síntese química
Antagonistas do Receptor A2 de Adenosina/química
Animais
Relação Dose-Resposta a Droga
Estrutura Molecular
Ratos
Relação Estrutura-Atividade
Tetralonas/síntese química
Tetralonas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adenosine A1 Receptor Antagonists); 0 (Adenosine A2 Receptor Antagonists); 0 (Receptor, Adenosine A1); 0 (Receptor, Adenosine A2A); 0 (Tetralones)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170908
[St] Status:MEDLINE


  2 / 284 MEDLINE  
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[PMID]:28374540
[Au] Autor:V PK; J R; C T FS; K T A; S Keri R; Varughese S; Balappa Somappa S
[Ad] Endereço:Academy of Scientific and Innovative Research (AcSIR), New Delhi, India.
[Ti] Título:Antibacterial and antitubercular evaluation of dihydronaphthalenone-indole hybrid analogs.
[So] Source:Chem Biol Drug Des;90(5):703-708, 2017 Nov.
[Is] ISSN:1747-0285
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A new series of indole appended dihydronaphthalenone hybrid analogs (5a-t) have been synthesized through the Lewis acid catalyzed Michael addition of indoles to the arylidene/hetero arylidene ketones. All the synthesized derivatives are well characterized through the H-NMR, C-NMR, HRMS spectroscopic techniques, compound 5r was further confirmed through single crystal X-ray analysis and screened for antibacterial and antitubercular activities. Among the synthesized compounds, the minimum inhibition concentration of 5l (against Escherichia coli) and 5o & 5p (against E. coli & Staphylococcus aureus) was found to be as low as 3.12 µg/ml as compared to the standard antibacterial drug ciprofloxacin 2.5 µg/ml. In antitubercular activity, compounds 5o and 5p with minimum inhibition concentration 6.25 µg/ml were found to be comparable with that of the drugs Pyrazinamide 5 µg/ml and Streptomycin 5 µg/ml. Compounds 5i, 5j, 5m, 5n, 5q, and 5r also showed promising activity against group of organisms tested.
[Mh] Termos MeSH primário: Antibacterianos/química
Antibacterianos/farmacologia
Bactérias/efeitos dos fármacos
Indóis/química
Indóis/farmacologia
Tetralonas/química
Tetralonas/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antituberculosos/síntese química
Antituberculosos/química
Antituberculosos/farmacologia
Infecções Bacterianas/tratamento farmacológico
Escherichia coli/efeitos dos fármacos
Seres Humanos
Indóis/síntese química
Testes de Sensibilidade Microbiana
Modelos Moleculares
Mycobacterium tuberculosis/efeitos dos fármacos
Staphylococcus aureus/efeitos dos fármacos
Relação Estrutura-Atividade
Tetralonas/síntese química
Tuberculose/tratamento farmacológico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antitubercular Agents); 0 (Indoles); 0 (Tetralones); 530-93-8 (beta-tetralone)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171113
[Lr] Data última revisão:
171113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170405
[St] Status:MEDLINE
[do] DOI:10.1111/cbdd.12990


  3 / 284 MEDLINE  
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[PMID]:27780313
[Au] Autor:Ceylan M; Kocyigit UM; Usta NC; Gürbüzlü B; Temel Y; Alwasel SH; Gülçin I
[Ad] Endereço:Department of Chemistry, Faculty of Arts and Sciences, Gaziosmanpasa University, Tokat, 60250, Turkey.
[Ti] Título:Synthesis, carbonic anhydrase I and II isoenzymes inhibition properties, and antibacterial activities of novel tetralone-based 1,4-benzothiazepine derivatives.
[So] Source:J Biochem Mol Toxicol;31(4), 2017 Apr.
[Is] ISSN:1099-0461
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Benzothiazepine compounds have a wide range of applications such as antibacterial, antidepressants, anticonvulsants, antihypertensives, antibiotics, antifungal, hypnotic, enzyme inhibitors, antitumor, anticancer and anti-HIV agents. In this study, the synthesis of novel tetralone-based benzothiazepine derivatives (1-16) and their in vitro antibacterial activity and human carbonic anhydrase isoenzymes I and II (hCA I and II) inhibitory effects were investigated. Both isoenzymes were purified by sepharose-4B-l-tyrosine-sulfanilamide affinity chromatography from fresh human red blood cells. All compounds demonstrated the low nanomolar inhibitory effects on both isoenzymes using esterase activity. Benzothiazepine derivative 2 demonstrated the best hCA I inhibitory effect with K value of 18.19 nM. Also, benzothiazepine derivative 7 showed the best hCA II inhibitory effect with K value of 11.31 nM. On the other hand, acetazolamide clinically used as CA inhibitor, showed K value of 19.92 nM against hCA I and 33.60 nM against hCA II, respectively.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Inibidores da Anidrase Carbônica/farmacologia
Tetralonas/farmacologia
Tiazepinas/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Anidrase Carbônica I/antagonistas & inibidores
Anidrase Carbônica I/isolamento & purificação
Anidrase Carbônica II/antagonistas & inibidores
Anidrase Carbônica II/isolamento & purificação
Inibidores da Anidrase Carbônica/síntese química
Eritrócitos/enzimologia
Seres Humanos
Tetralonas/síntese química
Tiazepinas/síntese química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Carbonic Anhydrase Inhibitors); 0 (Tetralones); 0 (Thiazepines); EC 4.2.1.- (Carbonic Anhydrase I); EC 4.2.1.- (Carbonic Anhydrase II)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170728
[Lr] Data última revisão:
170728
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161026
[St] Status:MEDLINE
[do] DOI:10.1002/jbt.21872


  4 / 284 MEDLINE  
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[PMID]:27806379
[Au] Autor:Xia Y; Lu G; Liu P; Dong G
[Ad] Endereço:Department of Chemistry, University of Texas at Austin, Austin, Texas 78712, USA.
[Ti] Título:Catalytic activation of carbon-carbon bonds in cyclopentanones.
[So] Source:Nature;539(7630):546-550, 2016 11 24.
[Is] ISSN:1476-4687
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In the chemical industry, molecules of interest are based primarily on carbon skeletons. When synthesizing such molecules, the activation of carbon-carbon single bonds (C-C bonds) in simple substrates is strategically important: it offers a way of disconnecting such inert bonds, forming more active linkages (for example, between carbon and a transition metal) and eventually producing more versatile scaffolds. The challenge in achieving such activation is the kinetic inertness of C-C bonds and the relative weakness of newly formed carbon-metal bonds. The most common tactic starts with a three- or four-membered carbon-ring system, in which strain release provides a crucial thermodynamic driving force. However, broadly useful methods that are based on catalytic activation of unstrained C-C bonds have proven elusive, because the cleavage process is much less energetically favourable. Here we report a general approach to the catalytic activation of C-C bonds in simple cyclopentanones and some cyclohexanones. The key to our success is the combination of a rhodium pre-catalyst, an N-heterocyclic carbene ligand and an amino-pyridine co-catalyst. When an aryl group is present in the C3 position of cyclopentanone, the less strained C-C bond can be activated; this is followed by activation of a carbon-hydrogen bond in the aryl group, leading to efficient synthesis of functionalized α-tetralones-a common structural motif and versatile building block in organic synthesis. Furthermore, this method can substantially enhance the efficiency of the enantioselective synthesis of some natural products of terpenoids. Density functional theory calculations reveal a mechanism involving an intriguing rhodium-bridged bicyclic intermediate.
[Mh] Termos MeSH primário: Carbono/química
Técnicas de Química Sintética
Ciclopentanos/química
[Mh] Termos MeSH secundário: Produtos Biológicos/síntese química
Produtos Biológicos/química
Catálise
Cicloexanonas/química
Ligações de Hidrogênio
Metano/análogos & derivados
Metano/química
Estrutura Molecular
Piridinas/química
Teoria Quântica
Ródio/química
Terpenos/síntese química
Terpenos/química
Tetralonas/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 (Biological Products); 0 (Cyclohexanones); 0 (Cyclopentanes); 0 (Pyridines); 0 (Terpenes); 0 (Tetralones); 220W81TN3S (cyclopentanone); 2465-56-7 (carbene); 7440-44-0 (Carbon); DMK383DSAC (Rhodium); NH9L3PP67S (pyridine); OP0UW79H66 (Methane)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161105
[St] Status:MEDLINE
[do] DOI:10.1038/nature19849


  5 / 284 MEDLINE  
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[PMID]:27467713
[Au] Autor:Tsasi G; Milosevic-Ifantis T; Skaltsa H
[Ad] Endereço:Division of Pharmacognosy & Chemistry of Natural Compounds, School of Pharmacy, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, GR-157 71, Athens.
[Ti] Título:Phytochemical Study of Juglans regia L. Pericarps from Greece with a Chemotaxonomic Approach.
[So] Source:Chem Biodivers;13(12):1636-1640, 2016 Dec.
[Is] ISSN:1612-1880
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Phytochemical research of different polarity extracts from green Juglans regia L. pericarps from Greece afforded 32 compounds: four pentacyclic triterpenes (1 - 4), three sesquiterpenes (5 - 7), four tetralones (8 - 11), two naphthoquinones (12 and 13), seven phenolic acids (14 - 20), one diarylheptanoid (21), one neo-lignan (22), seven flavonoids (23 - 29), two phenylethanoids (30 and 31) and one hydrolysed tannin (32). Compounds 4 and 29 are isolated for the first time from the species, while compounds 3, 7, 20, 22, 23, 24, 25, 26, 28, 30 are reported for the first time in Juglandaceae. Chemotaxonomic significance of isolated compounds into Junglandaceae family is thoroughly discussed.
[Mh] Termos MeSH primário: Juglans/química
Juglans/classificação
[Mh] Termos MeSH secundário: Grécia
Naftoquinonas/química
Naftoquinonas/isolamento & purificação
Compostos Fitoquímicos/química
Compostos Fitoquímicos/isolamento & purificação
Sesquiterpenos/química
Sesquiterpenos/isolamento & purificação
Tetralonas/química
Tetralonas/isolamento & purificação
Triterpenos/química
Triterpenos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Naphthoquinones); 0 (Phytochemicals); 0 (Sesquiterpenes); 0 (Tetralones); 0 (Triterpenes)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170120
[Lr] Data última revisão:
170120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160729
[St] Status:MEDLINE
[do] DOI:10.1002/cbdv.201600067


  6 / 284 MEDLINE  
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[PMID]:27434226
[Au] Autor:Leng J; Qin HL; Zhu K; Jantan I; Hussain MA; Sher M; Amjad MW; Naeem-Ul-Hassan M; Ahmad W; Bukhari SN
[Ad] Endereço:Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, Wuhan, China.
[Ti] Título:Evaluation of multifunctional synthetic tetralone derivatives for treatment of Alzheimer's disease.
[So] Source:Chem Biol Drug Des;88(6):889-898, 2016 Dec.
[Is] ISSN:1747-0285
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Neurodegeneration, a complex disease state, comprises several pathways that contribute to cell death. Conventional approach of targeting only one of these pathways has not been proven to be entirely successful and has demanded a hypothetical change as to how researchers design and develop new drugs. In this study, effects of a series of α, ß-unsaturated carbonyl-based tetralone derivatives against Alzheimer's disease (AD) were investigated. Moreover, their activity toward amyloid ß-induced cytotoxicity was also studied. Six compounds including 3f, 3o, 3u, 3ae, 3af, and 3ag were discovered to be most protective against Aß-induced neuronal cell death in PC12 cells. The findings of in vitro experiment revealed that most of these compounds exhibited potent inhibitory activity against MAO-B, AChE, and self-induced Aß aggregation. The compound 3f exhibited best AChE (IC  = 0.045 ± 0.02 µm) inhibitory potential in addition to potent inhibition of MAO-B (IC  = 0.88 ± 0.12 µm). Furthermore, compound 3f disassembled the Aß fibrils produced by self-induced Aß aggregation by 78.2 ± 4.8%. Collectively, these findings suggest that some compounds from this series have potential to be promising multifunctional agents for AD treatment.
[Mh] Termos MeSH primário: Doença de Alzheimer/tratamento farmacológico
Avaliação Pré-Clínica de Medicamentos
Tetralonas/uso terapêutico
[Mh] Termos MeSH secundário: Acetilcolinesterase/efeitos dos fármacos
Peptídeos beta-Amiloides/toxicidade
Animais
Butirilcolinesterase/efeitos dos fármacos
Espectroscopia de Ressonância Magnética Nuclear de Carbono-13
Inibidores da Colinesterase/uso terapêutico
Inibidores da Monoaminoxidase/uso terapêutico
Fármacos Neuroprotetores/uso terapêutico
Células PC12
Espectroscopia de Prótons por Ressonância Magnética
Ratos
Espectrometria de Massas por Ionização por Electrospray
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amyloid beta-Peptides); 0 (Cholinesterase Inhibitors); 0 (Monoamine Oxidase Inhibitors); 0 (Neuroprotective Agents); 0 (Tetralones); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160720
[St] Status:MEDLINE
[do] DOI:10.1111/cbdd.12822


  7 / 284 MEDLINE  
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[PMID]:27319147
[Au] Autor:Vera WJ; Banerjee AK
[Ti] Título:Synthesis of 5-Methoxy-6-isopropyl-1-tetralone.
[So] Source:Nat Prod Commun;11(5):671-2, 2016 May.
[Is] ISSN:1934-578X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:1-Hydroxytetralin was converted into 5-methoxy-6-isopropyl-1-tetralone in six steps.
[Mh] Termos MeSH primário: Tetralonas/química
[Mh] Termos MeSH secundário: Tetralonas/síntese química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (5-methoxy-6-isopropyl-1-tetralone); 0 (Tetralones)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:160620
[Lr] Data última revisão:
160620
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160621
[St] Status:MEDLINE


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[PMID]:27110760
[Au] Autor:Yang L; Ma XY; Ruan X; Jiang DA; Pan CD; Wang Q
[Ad] Endereço:Ningbo Institute of Technology, Zhejiang University, Ningbo 315100, China. yangli0817@yeah.net.
[Ti] Título:Enantioselective Separation of 4,8-DHT and Phytotoxicity of the Enantiomers on Various Plant Species.
[So] Source:Molecules;21(4):528, 2016 Apr 22.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:As a candidate for bioherbicide, 4,8-dihydroxy-1-tetralone (4,8-DHT) was isolated from Caryospora callicarpa epicarp and its two enantiomers, S-(+)-isosclerone and R-(-)-regiolone, were separated by chiral high-performance liquid chromatography (HPLC) on a Chiralcel OD column with chiral stationary phase (CSP)-coated cellulose-tris(3,5-dimethylphenylcarbamate). Then, the phytotoxicity of 4,8-DHT and its enantiomers toward the seeds germination and seedling growth of the five tested plant species, including lettuce (Latuca sativa), radish (Raphanus sativus), cucumber (Cucumis sativus), onion (Allium cepa), and wheat (Triticum aestivum), were investigated and the results indicated a hormesis at low concentration of 4,8-DHT and its enantiomers, but a retardant effect at high concentration. Between the two enantiomers of 4,8-DHT, the S-(+)-isosclerone was more toxic to seeds germination and seedling growth of the five tested plant species than the R-(-)-regiolone, and also the phytotoxicity of S-(+)-isosclerone varied with different plants. For example, S-(+)-isosclerone was the most active to seedling growth of lettuce, indicating that S-(+)-isosclerone had specific effects on different organisms. Thus, all of the chirality and concentration of 4,8-DHT, as well as the affected plant species, need to be taken into consideration in the development and utilization of 4,8-DHT.
[Mh] Termos MeSH primário: Coccídios/química
Produtos Agrícolas/efeitos dos fármacos
Produtos Agrícolas/crescimento & desenvolvimento
Herbicidas/toxicidade
Tetralonas/toxicidade
[Mh] Termos MeSH secundário: Cucumis sativus/efeitos dos fármacos
Cucumis sativus/crescimento & desenvolvimento
Germinação/efeitos dos fármacos
Herbicidas/isolamento & purificação
Alface/efeitos dos fármacos
Alface/crescimento & desenvolvimento
Cebolas/efeitos dos fármacos
Cebolas/crescimento & desenvolvimento
Raphanus/efeitos dos fármacos
Raphanus/crescimento & desenvolvimento
Plântulas/efeitos dos fármacos
Estereoisomerismo
Tetralonas/isolamento & purificação
Triticum/efeitos dos fármacos
Triticum/crescimento & desenvolvimento
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Herbicides); 0 (Tetralones)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170104
[Lr] Data última revisão:
170104
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160426
[St] Status:MEDLINE


  9 / 284 MEDLINE  
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[PMID]:27043213
[Au] Autor:Li X; Liu X; Jiao X; Yang H; Yao Y; Xie P
[Ad] Endereço:State Key Laboratory of Bioactive Substance and Function of Natural Medicine, Beijing Key Laboratory of Active Substance Discovery and Drugability Evaluation, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences , No. 1 Xiannongtan Street, Beijing 100050,
[Ti] Título:An approach to (±)-Lingzhiol.
[So] Source:Org Lett;18(8):1944-6, 2016 Apr 15.
[Is] ISSN:1523-7052
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:(±)-Lingzhiol has been synthesized from commercially available 5,8-dimethoxytetralone in seven steps with an overall yield of 10.3% via an unprecedented acid-catalyzed semipinacol-type rearrangement. In addition, a novel strategy for the construction of the tetracyclic 5/5/6/6 core structure of lingzhiol has been developed via a tandem rearrangement/reduction/lactonization reaction.
[Mh] Termos MeSH primário: Terpenos/síntese química
[Mh] Termos MeSH secundário: Catálise
Ciclização
Cicloexenos/química
Estrutura Molecular
Terpenos/química
Tetralonas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (5,8-dimethoxytetralone); 0 (Cyclohexenes); 0 (Terpenes); 0 (Tetralones); 0 (lingzhiol); 0 (semipinacol)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:160415
[Lr] Data última revisão:
160415
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160405
[St] Status:MEDLINE
[do] DOI:10.1021/acs.orglett.6b00542


  10 / 284 MEDLINE  
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[PMID]:27010345
[Au] Autor:Qin HL; Leng J; Zhang CP; Jantan I; Amjad MW; Sher M; Naeem-Ul-Hassan M; Hussain MA; Bukhari SN
[Ad] Endereço:Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology , 205 Luoshi Road, Wuhan 430070, P.R. China.
[Ti] Título:Synthesis of α,ß-Unsaturated Carbonyl-Based Compounds, Oxime and Oxime Ether Analogs as Potential Anticancer Agents for Overcoming Cancer Multidrug Resistance by Modulation of Efflux Pumps in Tumor Cells.
[So] Source:J Med Chem;59(7):3549-61, 2016 Apr 14.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Sixty-nine novel α,ß-unsaturated carbonyl based compounds, including cyclohexanone, tetralone, oxime, and oxime ether analogs, were synthesized. The antiproliferative activity determined by using seven different human cancer cell lines provided a structure-activity relationship. Compound 8ag exhibited high antiproliferative activity against Panc-1, PaCa-2, A-549, and PC-3 cell lines, with IC50 value of 0.02 µM, comparable to the positive control Erlotinib. The ten most active antiproliferative compounds were assessed for mechanistic effects on BRAF(V600E), EGFR TK kinases, and tubulin polymerization, and were investigated in vitro to reverse efflux-mediated resistance developed by cancer cells. Compound 8af exhibited the most potent BRAF(V600E) inhibitory activity with an IC50 value of 0.9 µM. Oxime analog 7o displayed the most potent EGFR TK inhibitory activity with an IC50 of 0.07 µM, which was analogous to the positive control. Some analogs including 7f, 8af, and 8ag showed a dual role as anticancer and MDR reversal agents.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Antineoplásicos/farmacologia
Cicloexanonas/química
Resistência a Múltiplos Medicamentos/efeitos dos fármacos
Éteres/química
Neoplasias/tratamento farmacológico
Oximas/química
Piperidonas/síntese química
Piperidonas/farmacologia
Tetralonas/síntese química
Tetralonas/farmacologia
[Mh] Termos MeSH secundário: Proliferação Celular/efeitos dos fármacos
Seres Humanos
Modelos Moleculares
Mutação/genética
Neoplasias/patologia
Oximas/síntese química
Oximas/farmacologia
Proteínas Proto-Oncogênicas B-raf/antagonistas & inibidores
Proteínas Proto-Oncogênicas B-raf/genética
Receptor do Fator de Crescimento Epidérmico/antagonistas & inibidores
Relação Estrutura-Atividade
Tubulina (Proteína)/química
Moduladores de Tubulina/síntese química
Moduladores de Tubulina/farmacologia
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (2-(2-chloro-3,4-dimethoxybenzylidene)-8-nitrotetralone oxime); 0 (3,5-bis(2-bromo-3,4,5-trimethoxybenzylidene)-1-methylpiperidin-4-one oxime); 0 (Antineoplastic Agents); 0 (Cyclohexanones); 0 (Ethers); 0 (Oximes); 0 (Piperidones); 0 (Tetralones); 0 (Tubulin); 0 (Tubulin Modulators); 5QOR3YM052 (cyclohexanone); EC 2.7.10.1 (EGFR protein, human); EC 2.7.10.1 (Receptor, Epidermal Growth Factor); EC 2.7.11.1 (BRAF protein, human); EC 2.7.11.1 (Proto-Oncogene Proteins B-raf)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:160415
[Lr] Data última revisão:
160415
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160325
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.6b00276



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