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Pesquisa : D02.455.426.559.847.389.850 [Categoria DeCS]
Referências encontradas : 323 [refinar]
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[PMID]:29227073
[Au] Autor:Uspenska KR; Gergalova GL; Lykhmus OY; Skok MV
[Ti] Título:The effect of amixin and agmatine on cytochrome C release from isolated mitochondria
[So] Source:Ukr Biochem J;88(1):5-10, 2016 Jan-Feb.
[Is] ISSN:2409-4943
[Cp] País de publicação:Ukraine
[La] Idioma:eng
[Ab] Resumo:Mitochondrial nicotinic acetylcholine receptors (nAChRs) control permeability transition pore formation and cytochrome c release in the presence of apoptogenic factors. This study demonstrates that pharmacological agents amixin and agmatine affect mitochondrial nAChR functioning: they slightly suppress cytochrome c release from mouse brain and liver mitochondria stimulated with apoptogenic dose of Са2+ and prevent the effect of α7 nAChR agonist PNU282987. We conclude that mitochondria may be one of therapeutic targets of amixin and agmatine.
[Mh] Termos MeSH primário: Agmatina/farmacologia
Indutores de Interferon/farmacologia
Mitocôndrias/efeitos dos fármacos
Tilorona/farmacologia
Receptor Nicotínico de Acetilcolina alfa7/metabolismo
[Mh] Termos MeSH secundário: Animais
Benzamidas/antagonistas & inibidores
Benzamidas/farmacologia
Encéfalo/efeitos dos fármacos
Compostos Bicíclicos com Pontes/antagonistas & inibidores
Compostos Bicíclicos com Pontes/farmacologia
Cálcio/farmacologia
Fracionamento Celular
Citocromos c/antagonistas & inibidores
Citocromos c/secreção
Fígado/efeitos dos fármacos
Fígado/metabolismo
Camundongos
Camundongos Endogâmicos C57BL
Mitocôndrias/metabolismo
Agonistas Nicotínicos/farmacologia
Especificidade de Órgãos
Receptor Nicotínico de Acetilcolina alfa7/agonistas
Receptor Nicotínico de Acetilcolina alfa7/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzamides); 0 (Bridged Bicyclo Compounds); 0 (Interferon Inducers); 0 (Nicotinic Agonists); 0 (PNU-282987); 0 (alpha7 Nicotinic Acetylcholine Receptor); 70J407ZL5Q (Agmatine); 9007-43-6 (Cytochromes c); O6W7VEW6KS (Tilorone); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180116
[Lr] Data última revisão:
180116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171212
[St] Status:MEDLINE
[do] DOI:10.15407/ubj88.01.005


  2 / 323 MEDLINE  
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[PMID]:27809794
[Au] Autor:Head BM; Rubinstein E; Meyers AF
[Ad] Endereço:Department of Medical Microbiology and Infectious Diseases, University of Manitoba, Winnipeg, MB, R3E 0J9, Canada. umheadb@outlook.com.
[Ti] Título:Alternative pre-approved and novel therapies for the treatment of anthrax.
[So] Source:BMC Infect Dis;16(1):621, 2016 Nov 03.
[Is] ISSN:1471-2334
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Bacillus anthracis, the causative agent of anthrax, is a spore forming and toxin producing rod-shaped bacterium that is classified as a category A bioterror agent. This pathogenic microbe can be transmitted to both animals and humans. Clinical presentation depends on the route of entry (direct contact, ingestion, injection or aerosolization) with symptoms ranging from isolated skin infections to more severe manifestations such as cardiac or pulmonary shock, meningitis, and death. To date, anthrax is treatable if antibiotics are administered promptly and continued for 60 days. However, if treatment is delayed or administered improperly, the patient's chances of survival are decreased drastically. In addition, antibiotics are ineffective against the harmful anthrax toxins and spores. Therefore, alternative therapeutics are essential. In this review article, we explore and discuss advances that have been made in anthrax therapy with a primary focus on alternative pre-approved and novel antibiotics as well as anti-toxin therapies. METHODS: A literature search was conducted using the University of Manitoba search engine. Using this search engine allowed access to a greater variety of journals/articles that would have otherwise been restricted for general use. In order to be considered for discussion for this review, all articles must have been published later than 2009. RESULTS: The alternative pre-approved antibiotics demonstrated high efficacy against B. anthracis both in vitro and in vivo. In addition, the safety profile and clinical pharmacology of these drugs were already known. Compounds that targeted underexploited bacterial processes (DNA replication, RNA synthesis, and cell division) were also very effective in combatting B. anthracis. In addition, these novel compounds prevented bacterial resistance. Targeting B. anthracis virulence, more specifically the anthrax toxins, increased the length of which treatment could be administered. CONCLUSIONS: Several novel and pre-existing antibiotics, as well as toxin inhibitors, have shown increasing promise. A combination treatment that targets both bacterial growth and toxin production would be ideal and probably necessary for effectively combatting this armed bacterium.
[Mh] Termos MeSH primário: Antraz/tratamento farmacológico
Antibacterianos/uso terapêutico
Antitoxinas/uso terapêutico
[Mh] Termos MeSH secundário: alfa-Globulinas/uso terapêutico
Antibióticos Antineoplásicos/uso terapêutico
Anticorpos Monoclonais/uso terapêutico
Antígenos de Bactérias
Bacillus anthracis
Toxinas Bacterianas
DNA Helicases/antagonistas & inibidores
Daunorrubicina/análogos & derivados
Daunorrubicina/uso terapêutico
Doxorrubicina/uso terapêutico
Descoberta de Drogas
Fluoroquinolonas
Seres Humanos
Indutores de Interferon/uso terapêutico
Levofloxacino
Linezolida
Ofloxacino
Policetídeos/uso terapêutico
Inibidores de Serino Proteinase/uso terapêutico
Tilorona/uso terapêutico
Virulência
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Alpha-Globulins); 0 (Anti-Bacterial Agents); 0 (Antibiotics, Antineoplastic); 0 (Antibodies, Monoclonal); 0 (Antigens, Bacterial); 0 (Antitoxins); 0 (Bacterial Toxins); 0 (Fluoroquinolones); 0 (Interferon Inducers); 0 (Polyketides); 0 (Serine Proteinase Inhibitors); 0 (anthracimycin); 0 (anthrax toxin); 29Z5DNL48C (obiltoxaximab); 39346-44-6 (inter-alpha-inhibitor); 64314-28-9 (baumycins); 6GNT3Y5LMF (Levofloxacin); 794PGL549S (raxibacumab); 80168379AG (Doxorubicin); A4P49JAZ9H (Ofloxacin); EC 3.6.4.- (DNA Helicases); ISQ9I6J12J (Linezolid); O6W7VEW6KS (Tilorone); U188XYD42P (moxifloxacin); ZS7284E0ZP (Daunorubicin)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161105
[St] Status:MEDLINE


  3 / 323 MEDLINE  
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[PMID]:26633340
[Au] Autor:Zhang J; Yao Q; Liu Z
[Ad] Endereço:School of Chemical Engineering, Nanjing University of Science and Technology, Nanjing 210094, China. zjr1108@njau.edu.cn.
[Ti] Título:An Effective Synthesis Method for Tilorone Dihydrochloride with Obvious IFN-α Inducing Activity.
[So] Source:Molecules;20(12):21458-63, 2015 Dec 02.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Tilorone dihydrochloride (1) has great potential for inducing interferon against pathogenic infection. In this paper, we describe a convenient preparation method for 2,7-dihydroxyfluoren-9-one (2), which is a usual pharmaceutical intermediate for preparing tilorone dihydrochloride (1). In the novel method, methyl esterification of 4,4'-dihydroxy-[1,1'-biphenyl]-2-carboxylic acid (4) was carried out under milder conditions with higher yield and played an important role in the preparation of compound 2. The structures of the relative intermediates and target compound were characterized by melting point, IR, MS, and ¹H-NMR. Furthermore, the synthesized tilorone dihydrochloride exhibited an obvious effect on induction of interferon-α (IFN-α) in mice within 12 h, and the peak level was observed until 24 h. This fruitful work has resulted in tilorone dihydrochloride becoming available in large-scale and wide application in clinics, which has a good pharmaceutical development prospects.
[Mh] Termos MeSH primário: Indutores de Interferon/síntese química
Indutores de Interferon/farmacologia
Interferon-alfa/metabolismo
Tilorona/síntese química
Tilorona/farmacologia
[Mh] Termos MeSH secundário: Animais
Camundongos
Espectroscopia de Prótons por Ressonância Magnética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Interferon Inducers); 0 (Interferon-alpha); O6W7VEW6KS (Tilorone)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:151204
[Lr] Data última revisão:
151204
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151204
[St] Status:MEDLINE
[do] DOI:10.3390/molecules201219781


  4 / 323 MEDLINE  
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[PMID]:24841903
[Au] Autor:Wissing MD; Dadon T; Kim E; Piontek KB; Shim JS; Kaelber NS; Liu JO; Kachhap SK; Nelkin BD
[Ad] Endereço:Department of Oncology, Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University School of Medicine, Baltimore, MD 21287, USA.
[Ti] Título:Small-molecule screening of PC3 prostate cancer cells identifies tilorone dihydrochloride to selectively inhibit cell growth based on cyclin-dependent kinase 5 expression.
[So] Source:Oncol Rep;32(1):419-24, 2014 Jul.
[Is] ISSN:1791-2431
[Cp] País de publicação:Greece
[La] Idioma:eng
[Ab] Resumo:Cyclin-dependent kinase 5 (CDK5) is a potential target for prostate cancer treatment, the enzyme being essential for prostate tumor growth and formation of metastases. In the present study, we identified agents that target prostate cancer cells based on CDK5 expression. CDK5 activity was suppressed by transfection of PC3 prostate cancer cells with a dominant-negative construct (PC3 CDK5dn). PC3 CDK5dn and PC3 control cells were screened for compounds that selectively target cells based on CDK5 expression, utilizing the Johns Hopkins Drug Library. MTS proliferation, clonogenic and 3D growth assays were performed to validate the selected hits. Screening of 3,360 compounds identified rutilantin, ethacridine lactate and cetalkonium chloride as compounds that selectively target PC3 control cells and a tilorone analog as a selective inhibitor of PC3 CDK5dn cells. A PubMed literature study indicated that tilorone may have clinical use in patients. Validation experiments confirmed that tilorone treatment resulted in decreased PC3 cell growth and invasion; PC3 cells with inactive CDK5 were inhibited more effectively. Future studies are needed to unravel the mechanism of action of tilorone in CDK5 deficient prostate cancer cells and to test combination therapies with tilorone and a CDK5 inhibitor for its potential use in clinical practice.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Quinase 5 Dependente de Ciclina/metabolismo
Invasividade Neoplásica/patologia
Neoplasias da Próstata/patologia
Tilorona/farmacologia
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos
Seres Humanos
Masculino
Neoplasias da Próstata/metabolismo
Bibliotecas de Moléculas Pequenas/farmacologia
[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 (Small Molecule Libraries); EC 2.7.11.1 (Cyclin-Dependent Kinase 5); EC 2.7.11.22 (CDK5 protein, human); O6W7VEW6KS (Tilorone)
[Em] Mês de entrada:1501
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140521
[St] Status:MEDLINE
[do] DOI:10.3892/or.2014.3174


  5 / 323 MEDLINE  
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[PMID]:24273882
[Au] Autor:Chen L; Wang F
[Ad] Endereço:Tianjin Medical University, No. 220, Dongting Road, 300 457 Tianjin, PR China. cliangmei@gmail.com
[Ti] Título:Development of sustained-release matrix tablets of BKP-01-041 (tilorone derivative) containing Hypromellose.
[So] Source:Pharmazie;68(10):796-9, 2013 Oct.
[Is] ISSN:0031-7144
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The objective of this research was to develop and evaluate sustained-release matrix tablets of BKP-01-041 (tilorone derivative) based on Hypromellose (hydroxypropyl methylcellulose, HPMC) as the matrix forming polymer. The sustained-release tablets were prepared by the wet granulation method. The influence of HPMC viscosity and ratios on drug release was investigated in vitro. Dissolution of the tablets developed with 26% HPMC K4 M/K100 M (1:2) (w/w) content showed a better drug release profile than the other batches tested in 12 h. Drug release from the optimal formulation was analyzed using release kinetics equations. The release kinetics parameters were determined and the value of the exponent (n) representing the apparent drug release mechanism determined from the Peppas equation was about 0.726. These results suggest that the drug release mechanism was non-Fickian (0.45 < n < 0.89), and drug release was dependent on both drug diffusion and polymer erosion.
[Mh] Termos MeSH primário: Metilcelulose/análogos & derivados
Tilorona/análogos & derivados
Tilorona/administração & dosagem
[Mh] Termos MeSH secundário: Algoritmos
Química Farmacêutica
Preparações de Ação Retardada
Excipientes
Derivados da Hipromelose
Cinética
Metilcelulose/administração & dosagem
Metilcelulose/química
Pós
Solubilidade
Tilorona/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (BKP-01-041); 0 (Delayed-Action Preparations); 0 (Excipients); 0 (Powders); 3NXW29V3WO (Hypromellose Derivatives); 9004-67-5 (Methylcellulose); O6W7VEW6KS (Tilorone)
[Em] Mês de entrada:1401
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131127
[St] Status:MEDLINE


  6 / 323 MEDLINE  
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[PMID]:24094433
[Au] Autor:Lee CC; Chang DM; Huang KF; Chen CL; Chen TC; Lo Y; Guh JH; Huang HS
[Ad] Endereço:Graduate Institute of Life Sciences, National Defense Medical Center, Taipei 114, Taiwan; School of Pharmacy, National Defense Medical Center, Taipei 114, Taiwan.
[Ti] Título:Design, synthesis and antiproliferative evaluation of fluorenone analogs with DNA topoisomerase I inhibitory properties.
[So] Source:Bioorg Med Chem;21(22):7125-33, 2013 Nov 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of 2,7-diamidofluorenones were designed, synthesized, and screened by SRB assay. Some synthesized compounds exhibited antitumor activities in submicromolar range. Ten compounds (3a, 3b, 3c, 3g, 3j, 3l, 4a, 4h, 4i, and 4j) were also selected by NCI screening system and 3c (GI50=1.66 µM) appeared to be the most active agent of this series. Furthermore, 3c attenuated topoisomerase I-mediated DNA relaxation at low micromolar concentrations. These results indicated that fluorenones have potential to be further developed into anticancer drugs.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Antineoplásicos/farmacologia
DNA Topoisomerases Tipo I/química
Desenho de Drogas
Tilorona/análogos & derivados
Inibidores da Topoisomerase I/síntese química
Inibidores da Topoisomerase I/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
DNA Topoisomerases Tipo I/metabolismo
Seres Humanos
Relação Estrutura-Atividade
Tilorona/química
Tilorona/farmacologia
Inibidores da Topoisomerase I/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Topoisomerase I Inhibitors); EC 5.99.1.2 (DNA Topoisomerases, Type I); EC 5.99.1.2 (TOP1 protein, human); O6W7VEW6KS (Tilorone)
[Em] Mês de entrada:1405
[Cu] Atualização por classe:131016
[Lr] Data última revisão:
131016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131008
[St] Status:MEDLINE


  7 / 323 MEDLINE  
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[PMID]:24004110
[Au] Autor:Biswas T; Green KD; Garneau-Tsodikova S; Tsodikov OV
[Ad] Endereço:Department of Medicinal Chemistry, College of Pharmacy, University of Michigan , Ann Arbor, Michigan 48109, United States.
[Ti] Título:Discovery of inhibitors of Bacillus anthracis primase DnaG.
[So] Source:Biochemistry;52(39):6905-10, 2013 Oct 01.
[Is] ISSN:1520-4995
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Primase DnaG is an essential bacterial enzyme that synthesizes short ribonucleotide primers required for chromosomal DNA replication. Inhibitors of DnaG can serve as leads for development of new antibacterials and biochemical probes. We recently developed a nonradioactive in vitro primase-pyrophosphatase assay to identify and analyze DnaG inhibitors. Application of this assay to DnaG from Bacillus anthracis (Ba DnaG), a dangerous pathogen, yielded several inhibitors, which include agents with DNA intercalating properties (doxorubicin and tilorone) as well as those that do not intercalate into DNA (suramin). A polyanionic agent and inhibitor of eukaryotic primases, suramin, identified by this assay as a low-micromolar Ba DnaG inhibitor, was recently shown to be also a low-micromolar inhibitor of Mycobacterium tuberculosis DnaG (Mtb DnaG). In contrast, another low-micromolar Ba DnaG inhibitor, tilorone, is much more potent against Ba DnaG than against Mtb DnaG, despite homology between these enzymes, suggesting that DnaG can be targeted selectively.
[Mh] Termos MeSH primário: Bacillus anthracis/enzimologia
DNA Primase/antagonistas & inibidores
Descoberta de Drogas
Inibidores Enzimáticos/farmacologia
[Mh] Termos MeSH secundário: Animais
Células Cultivadas
DNA Primase/isolamento & purificação
DNA Primase/metabolismo
Doxorrubicina/química
Doxorrubicina/farmacologia
Inibidores Enzimáticos/química
Ensaios de Triagem em Larga Escala
Levofloxacino/química
Levofloxacino/farmacologia
Camundongos
Estrutura Molecular
Relação Estrutura-Atividade
Suramina/química
Suramina/farmacologia
Tilorona/química
Tilorona/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Enzyme Inhibitors); 6032D45BEM (Suramin); 6GNT3Y5LMF (Levofloxacin); 80168379AG (Doxorubicin); EC 2.7.7.- (DNA Primase); O6W7VEW6KS (Tilorone)
[Em] Mês de entrada:1401
[Cu] Atualização por classe:131002
[Lr] Data última revisão:
131002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130906
[St] Status:MEDLINE
[do] DOI:10.1021/bi4011286


  8 / 323 MEDLINE  
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[PMID]:23987044
[Au] Autor:Strel'tsova OS; Krupin VN; Rastorguev GG
[Ti] Título:[The role of immunomodulating therapy in the treatment and prevention of exacerbations of chronic cystitis].
[So] Source:Urologiia;(3):24-6, 28, 2013 May-Jun.
[Is] ISSN:1728-2985
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:The article presents the results of the examination and treatment of 60 women with chronic cystitis aged 20 to 80 years. The mean disease duration was 4,9 years (ranged from 6 months to 40 years). Immunomodulator Tilorone was included in the complex therapy of 30 patients of the main group. Besides the standard examination, immunological studies, including the definition of netrophil phagocytic rates in the patients were performed. It was revealed that the inclusion of immunomodulator in the treatment regimen of exacerbations of chronic cystitis contributes to an increase of index of activation of neutrophil phagocytic reserve, significant reduction in the frequency of exacerbations of the disease after the basic and preventive courses of treatment.
[Mh] Termos MeSH primário: Cistite Intersticial/terapia
Indutores de Interferon/administração & dosagem
Tilorona/administração & dosagem
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Cistite Intersticial/imunologia
Cistite Intersticial/patologia
Feminino
Seres Humanos
Meia-Idade
Neutrófilos/imunologia
Neutrófilos/patologia
Fagocitose/efeitos dos fármacos
Fagocitose/imunologia
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Interferon Inducers); O6W7VEW6KS (Tilorone)
[Em] Mês de entrada:1309
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130831
[St] Status:MEDLINE


  9 / 323 MEDLINE  
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[PMID]:23957162
[Au] Autor:Dolga OV; Pogoriela NKh; Bohorad-Kobel's'ka OS; Zholobak NM; Zanoza SO; Liakhov SA; Mahura IS
[Ti] Título:[Effects of diphenyl derivatives on electrophoretic mobility of murine T lymphocytes].
[So] Source:Fiziol Zh;59(3):31-8, 2013.
[Is] ISSN:2522-9028
[Cp] País de publicação:Ukraine
[La] Idioma:ukr
[Ab] Resumo:The early changes of electrophoretic mobility (EPM) of murine T lymphocytes induced by structural analogues of amixine-dihydrochloryde 4,4'-bis-[2(diethylamino)ethoxy]diphenyl (compound 1) and dihydrochloryde 2-methoxycarbonil-4,4'-bis-[2(diethylamino)ethoxy]diphenyl (compound 2) were studied by electrophoresis technique. During the interval 0-2 hours all compounds increased the absolute values of EPM in comparison with control. These changes were of the same kind--distinctions were quantitative. Amixine and compound 1 during the interval 2-4 hours additionally increased the EPM. The compound 2, on the contrary, decreased the EPM. It was shown that the opposite effects of the aforementioned compounds were caused by the fact that amixine and compound 1 induce, and compound 2 does not induce IFN production in T lymphocytes in vitro. The results of our experiments are important for understanding of the mechanisms of immunomodulating effect of amixine and its structural analogues.
[Mh] Termos MeSH primário: Compostos de Bifenilo/farmacologia
Fatores Imunológicos/farmacologia
Baço/efeitos dos fármacos
Linfócitos T/efeitos dos fármacos
Tilorona/farmacologia
[Mh] Termos MeSH secundário: Animais
Células Cultivadas
Relação Dose-Resposta a Droga
Eletroforese
Interferons/agonistas
Interferons/secreção
Masculino
Camundongos
Camundongos Endogâmicos CBA
Baço/citologia
Linfócitos T/citologia
Tilorona/análogos & derivados
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biphenyl Compounds); 0 (Immunologic Factors); 9008-11-1 (Interferons); O6W7VEW6KS (Tilorone)
[Em] Mês de entrada:1309
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130821
[St] Status:MEDLINE


  10 / 323 MEDLINE  
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[PMID]:23665799
[Au] Autor:Zhou D; Tuo W; Hu H; Xu J; Chen H; Rao Z; Xiao Y; Hu X; Liu P
[Ad] Endereço:State Key Laboratory of Virology, Ministry of Education Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, Wuhan 430071, China. zhoudingshan@whu.edu.cn
[Ti] Título:Synthesis and activity evaluation of tilorone analogs as potential anticancer agents.
[So] Source:Eur J Med Chem;64:432-41, 2013 Jun.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Tilorone is an interferon inducer with anticancer activity. Twenty-two novel tilorone analogs were synthesized by improvements of fluorenone skeleton, side chains and amino groups to screen new anticancer agents. In vitro evaluation showed that ten new compounds had better anticancer activities than tilorone. Among them, 2c (IC50 < 7 µM against cancer cell lines and IC50 > 35 µM against non-cancer cell lines) and 5d (IC50 < 10 µM against cancer cell lines and IC50 > 53 µM against non-cancer cell lines) exhibited the best anticancer activities and selectivities. Pharmacophore modeling of highly active compounds was carried out by Molecular Operating Environment (MOE) to generate a visualized model for compound design in future study.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Tilorona/farmacologia
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular
Proliferação Celular/efeitos dos fármacos
Cercopithecus aethiops
Relação Dose-Resposta a Droga
Avaliação Pré-Clínica de Medicamentos
Células HEK293
Células HeLa
Seres Humanos
Modelos Moleculares
Estrutura Molecular
Relação Estrutura-Atividade
Tilorona/síntese química
Tilorona/química
Células Vero
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); O6W7VEW6KS (Tilorone)
[Em] Mês de entrada:1311
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130514
[St] Status:MEDLINE



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