Base de dados : MEDLINE
Pesquisa : D03.633.100.473.525 [Categoria DeCS]
Referências encontradas : 771 [refinar]
Mostrando: 1 .. 10   no formato [Detalhado]

página 1 de 78 ir para página                         

  1 / 771 MEDLINE  
              next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29288946
[Au] Autor:Wang J; Yun D; Yao J; Fu W; Huang F; Chen L; Wei T; Yu C; Xu H; Zhou X; Huang Y; Wu J; Qiu P; Li W
[Ad] Endereço:Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical Universtiy, Wenzhou, Zhejiang 325035, China; Wenzhou Biomedical Innovation Center, Wenzhou University and Wenzhou Medical University, Wenzhou, Zhejiang 325035, China.
[Ti] Título:Design, synthesis and QSAR study of novel isatin analogues inspired Michael acceptor as potential anticancer compounds.
[So] Source:Eur J Med Chem;144:493-503, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Molecular hybridization is considered as an effective tactic to develop drugs for the treatment of cancer. A series of novel hybrid compounds of isatin and Michael acceptor were designed and synthesized on the basis of association principle. These hybrid compounds were tested for cytotoxic potential against human cancer cell lines namely, BGC-823, SGC-7901 and NCI-H460 by MTT assay. Most compounds showed good anti-growth activities in all tested human cancer cells. SAR and QSAR analysis may provide vital information for the future development of novel anti-cancer inhibitors. Notably, compound 6a showed potent growth inhibition on BGC-823, SGC-7901 and NCI-H460 with the IC values of 3.6 ±â€¯0.6, 5.7 ±â€¯1.2, 3.2 ±â€¯0.7 µM, respectively. Besides, colony formation assays, wound healing assays and flow cytometry analysis indicated 6a exhibited a potent anti-growth and anti-migration ability in a concentration-dependence manner through arrested cells in the G2/M phase of cell cycle. Moreover, 6a significantly repressed tumor growth in a NCI-H460 xenograft mouse model. Overall, our findings suggested isatin analogues inspired Michael acceptor may provide promising lead compounds for the development of cancer chemotherapeutics.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Desenho de Drogas
Isatina/farmacologia
Relação Quantitativa Estrutura-Atividade
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/síntese química
Antineoplásicos/química
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Isatina/síntese química
Isatina/química
Camundongos
Camundongos Endogâmicos BALB C
Camundongos Nus
Estrutura Molecular
Neoplasias Experimentais/tratamento farmacológico
Neoplasias Experimentais/patologia
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 82X95S7M06 (Isatin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171231
[St] Status:MEDLINE


  2 / 771 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29208524
[Au] Autor:Wang G; Chen M; Qiu J; Xie Z; Cao A
[Ad] Endereço:Provincial Key Laboratory of Pharmaceutics in Guizhou Province, Guizhou Medical University, 4 Beijing Road, Guiyang 550004, China; School of Pharmacy, Guizhou Medical University, 4 Beijing Road, Guiyang 550004, China; National Engineering Research Center of Miao's Medicines, 4 Beijing Road, Guiyang
[Ti] Título:Synthesis, in vitro α-glucosidase inhibitory activity and docking studies of novel chromone-isatin derivatives.
[So] Source:Bioorg Med Chem Lett;28(2):113-116, 2018 01 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A novel series of chromone-isatin derivatives 6a-6p were designed, synthesized and characterized by H NMR, C NMR and HRMS. These novel synthetic compounds were evaluated for inhibitory activity against yeast α-glucosidase enzyme. The results of biological test have shown that all tested compounds exhibited excellent to potent inhibitory activity in the range of IC = 3.18 ±â€¯0.12-16.59 ±â€¯0.17 µM as compared to the standard drug acarbose (IC = 817.38 ±â€¯6.27 µM). Compound 6j (IC = 3.18 ±â€¯0.12 µM) with a hydroxyl group at the 7-position of chromone and a 4-bromobenzyl group at the N1-positions of isatin, was found to be the most active compound among the series. Furthermore, molecular docking study was performed to help understand binding interactions of the most active analogs with α-glucosidase enzyme. These results indicated that this class of compounds had potential for the development of anti-diabetic agents.
[Mh] Termos MeSH primário: Cromonas/farmacologia
Inibidores de Glicosídeo Hidrolases/farmacologia
Isatina/farmacologia
Simulação de Acoplamento Molecular
alfa-Glucosidases/metabolismo
[Mh] Termos MeSH secundário: Cromonas/química
Relação Dose-Resposta a Droga
Inibidores de Glicosídeo Hidrolases/síntese química
Inibidores de Glicosídeo Hidrolases/química
Isatina/química
Estrutura Molecular
Saccharomyces cerevisiae/enzimologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Chromones); 0 (Glycoside Hydrolase Inhibitors); 82X95S7M06 (Isatin); EC 3.2.1.20 (alpha-Glucosidases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171207
[St] Status:MEDLINE


  3 / 771 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28923662
[Au] Autor:Kammoonah S; Prasad B; Balaraman P; Mundhada H; Schwaneberg U; Plettner E
[Ad] Endereço:Department of Chemistry, Simon Fraser University, 8888 University Drive, Burnaby, BC V5A 1S6, Canada.
[Ti] Título:Selecting of a cytochrome P450 SeSaM library with 3-chloroindole and endosulfan - Identification of mutants that dehalogenate 3-chloroindole.
[So] Source:Biochim Biophys Acta;1866(1):68-79, 2018 01.
[Is] ISSN:0006-3002
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Cytochrome P450 (a camphor hydroxylase) from the soil bacterium Pseudomonas putida shows potential importance in environmental applications such as the degradation of chlorinated organic pollutants. Seven P450 mutants generated from Sequence Saturation Mutagenesis (SeSaM) and isolated by selection on minimal media with either 3-chloroindole or the insecticide endosulfan were studied for their ability to oxidize of 3-chloroindole to isatin. The wild-type enzyme did not accept 3-chloroindole as a substrate. Mutant (E156G/V247F/V253G/F256S) had the highest maximal velocity in the conversion of 3-chloroindole to isatin, whereas mutants (T56A/N116H/D297N) and (G60S/Y75H) had highest k /K values. Six of the mutants had more than one mutation, and within this set, mutation of residues 297 and 179 was observed twice. Docking simulations were performed on models of the mutant enzymes; the wild-type did not accommodate 3-chloroindole in the active site, whereas all the mutants did. We propose two potential reaction pathways for dechlorination of 3-chloroindole. This article is part of a Special Issue entitled: Cytochrome P450 biodiversity and biotechnology, edited by Erika Plettner, Gianfranco Gilardi, Luet Wong, Vlada Urlacher, Jared Goldstone.
[Mh] Termos MeSH primário: Proteínas de Bactérias/química
Cânfora 5-Mono-Oxigenase/química
Endossulfano/metabolismo
Biblioteca Gênica
Indóis/metabolismo
Pseudomonas putida/enzimologia
[Mh] Termos MeSH secundário: Motivos de Aminoácidos
Substituição de Aminoácidos
Proteínas de Bactérias/genética
Proteínas de Bactérias/metabolismo
Sítios de Ligação
Biodegradação Ambiental
Cânfora 5-Mono-Oxigenase/genética
Cânfora 5-Mono-Oxigenase/metabolismo
Clonagem Molecular
Endossulfano/química
Escherichia coli/genética
Escherichia coli/metabolismo
Expressão Gênica
Halogenação
Indóis/química
Isatina/química
Isatina/metabolismo
Cinética
Simulação de Acoplamento Molecular
Mutação
Oxirredução
Ligação Proteica
Domínios e Motivos de Interação entre Proteínas
Estrutura Secundária de Proteína
Pseudomonas putida/química
Proteínas Recombinantes/química
Proteínas Recombinantes/genética
Proteínas Recombinantes/metabolismo
Especificidade por Substrato
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Bacterial Proteins); 0 (Indoles); 0 (Recombinant Proteins); 82X95S7M06 (Isatin); EC 1.14.15.1 (Camphor 5-Monooxygenase); OKA6A6ZD4K (Endosulfan)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180208
[Lr] Data última revisão:
180208
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170920
[St] Status:MEDLINE


  4 / 771 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29227930
[Au] Autor:Yan X; Lv Z; Wen J; Zhao S; Xu Z
[Ad] Endereço:College of Pharmacy, Harbin University of Commerce, Harbin, Heilongjiang Province 150076, PR China. Electronic address: yanxinjia@yeah.net.
[Ti] Título:Synthesis and in vitro evaluation of novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids for their anti-mycobacterial activities.
[So] Source:Eur J Med Chem;143:899-904, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Twelve novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids 5a-l were designed, synthesized and screened for their in vitro anti-mycobacterial activities against drug-sensitive and multidrug-resistant Mycobacterium tuberculosis as well as cytotoxicity in VERO cell line. All hybrids exhibited excellent activities against two Mycobacterium tuberculosis strains with minimum inhibitory concentration in the range from 0.05 to 2.0 µg/mL. The most active hybrid 5i was 2-8 times more potent than the reference agents (moxifloxacin and rifampicin) in vitro against Mycobacterium tuberculosis H Rv, while 2->2048 times more potent than the reference agents (moxifloxacin, rifampicin and isoniazid) in vitro against multidrug-resistant Mycobacterium tuberculosis. However, all hybrids (the 50% cytotoxic concentration/CC : 2-32 µg/mL) were much more cytotoxic than the parent moxifloxacin (CC : 128 µg/mL) against VERO cell line. Therefore, our further optimization will focus on their cytotoxicity reducing as well as activity enhancing. The structure-activity relationship of 1H-1,2,3-triazole-tethered isatin-fluoroquinolone hybrids was investigated, and the results could promote further development of the anti-tuberculosis properties of this kind of hybrids.
[Mh] Termos MeSH primário: Alcenos/farmacologia
Antibacterianos/farmacologia
Fluoroquinolonas/farmacologia
Isatina/farmacologia
Mycobacterium tuberculosis/efeitos dos fármacos
Triazóis/farmacologia
Tuberculose Resistente a Múltiplos Medicamentos/tratamento farmacológico
[Mh] Termos MeSH secundário: Alcenos/química
Animais
Antibacterianos/síntese química
Antibacterianos/química
Sobrevivência Celular/efeitos dos fármacos
Cercopithecus aethiops
Relação Dose-Resposta a Droga
Feminino
Fluoroquinolonas/química
Isatina/química
Camundongos
Camundongos Endogâmicos ICR
Testes de Sensibilidade Microbiana
Estrutura Molecular
Relação Estrutura-Atividade
Triazóis/química
Células Vero
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkenes); 0 (Anti-Bacterial Agents); 0 (Fluoroquinolones); 0 (Triazoles); 82X95S7M06 (Isatin); AUG1H506LY (propylene); U188XYD42P (moxifloxacin)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180101
[Lr] Data última revisão:
180101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171212
[St] Status:MEDLINE


  5 / 771 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28797799
[Au] Autor:Singh H; Singh JV; Gupta MK; Saxena AK; Sharma S; Nepali K; Bedi PMS
[Ad] Endereço:Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab 143005, India.
[Ti] Título:Triazole tethered isatin-coumarin based molecular hybrids as novel antitubulin agents: Design, synthesis, biological investigation and docking studies.
[So] Source:Bioorg Med Chem Lett;27(17):3974-3979, 2017 09 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In an attempt to develop potent anti-tubulin agents against most dreadful disease cancer, a library of 28 novel triazole tethered isatin-coumarin hybrids were synthesized by click chemistry approach. Synthesized hybrids were characterized and evaluated against a panel of human cancer cell lines viz. THP-1, COLO-205, HCT-116 and PC-3. Biological assay unveiled that, compounds A-1 to A-6, B-1 to B-4 and C-1 to C-3 displayed significant inhibitory potential against THP-1, COLO-205 and HCT-116 cell lines which were more sensitive towards the designed hybrids. PC-3 among these cell lines was found to be almost resistant. Established SAR revealed marked dependence of the cytotoxic activity on the type of substituent on isatin and the length of carbon-bridge connecting isatin moiety with triazole ring. Unsubstituted isatin and two carbon-bridge were found to be crucial for cytotoxicity. Three most potent hybrids (A-1, A-2 and B-1) were further tested for tubulin polymerization inhibition. Among these three compounds, A-1 found to be endowed with most prominent tubulin polymerization inhibition potential with IC value of 1.06µM which was further confirmed by using confocal microscopy. Possible binding interactions between the most potent hybrid molecule A-1 and tubulin were also divulged by molecular modeling studies.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Cumarínicos/farmacologia
Desenho de Drogas
Isatina/farmacologia
Triazóis/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Cumarínicos/química
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Isatina/química
Simulação de Acoplamento Molecular
Estrutura Molecular
Relação Estrutura-Atividade
Triazóis/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Coumarins); 0 (Triazoles); 82X95S7M06 (Isatin); A4VZ22K1WT (coumarin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170812
[St] Status:MEDLINE


  6 / 771 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28720502
[Au] Autor:Xu Z; Zhang S; Song X; Qiang M; Lv Z
[Ad] Endereço:Key Laboratory of Hubei Province for Coal Conversion and New Carbon Materials, Wuhan University of Science and Technology, Hubei, PR China.
[Ti] Título:Design, synthesis and in vitro anti-mycobacterial evaluation of gatifloxacin-1H-1,2,3-triazole-isatin hybrids.
[So] Source:Bioorg Med Chem Lett;27(16):3643-3646, 2017 08 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A set of novel gatifloxacin-1H-1,2,3-triazole-isatin hybrids 6a-l was designed, synthesized and evaluated for their in vitro anti-mycobacterial activities against M. tuberculosis (MTB) H Rv and MDR-TB as well as cytotoxicity. The results showed that all the targets (MIC: 0.025-3.12µg/mL) exhibited excellent inhibitory activity against MTB H Rv and MDR-TB, but were much more toxic (CC : 7.8-62.5µg/mL) than the parent gatifloxacin (GTFX) (CC : 125µg/mL). Among them, 61 (MIC: 0.025µg/mL) was 2-32 times more potent in vitro than the references INH (MIC: 0.05µg/mL), GTFX (MIC: 0.78µg/mL) and RIF (MIC: 0.39µg/mL) against MTB H Rv. The most active conjugate 6k (MIC: 0.06µg/mL) was 16->2048 times more potent than the three references (MIC: 1.0->128µg/mL) against MDR-TB. Both of the two hybrids warrant further investigations.
[Mh] Termos MeSH primário: Antituberculosos/química
Antituberculosos/farmacologia
Desenho de Drogas
Fluoroquinolonas/química
Isatina/química
Mycobacterium tuberculosis/efeitos dos fármacos
Triazóis/química
[Mh] Termos MeSH secundário: Antituberculosos/síntese química
Farmacorresistência Bacteriana/efeitos dos fármacos
Testes de Sensibilidade Microbiana
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antitubercular Agents); 0 (Fluoroquinolones); 0 (Triazoles); 82X95S7M06 (Isatin); L4618BD7KJ (gatifloxacin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170720
[St] Status:MEDLINE


  7 / 771 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28718672
[Au] Autor:El-Azab AS; Al-Dhfyan A; Abdel-Aziz AA; Abou-Zeid LA; Alkahtani HM; Al-Obaid AM; Al-Gendy MA
[Ad] Endereço:a Department of Pharmaceutical Chemistry , College of Pharmacy, King Saud University , Riyadh , Saudi Arabia.
[Ti] Título:Synthesis, anticancer and apoptosis-inducing activities of quinazoline-isatin conjugates: epidermal growth factor receptor-tyrosine kinase assay and molecular docking studies.
[So] Source:J Enzyme Inhib Med Chem;32(1):935-944, 2017 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A new series of quinazolinone compounds 16-34 incorporating isatin moieties was synthesized. The antitumor efficacy of the compounds against MDA-MB-231, a breast cancer cell line, and LOVO, a colon cancer cell line, was assessed. Compounds 20, 21, 22, 23, 25, 27, 28, 29, 30, 31, 32, 33, and 34 displayed potent antitumor activity against MDA-MB-231 and LOVO cells (IC : 10.38-38.67 µM and 9.91-15.77 µM, respectively); the comparative IC values for 5-fluorouracil and erlotinib in these cells lines were 70.28 µM, 22.24 µM and 15.23 µM, 25.31 µM respectively. The EGFR-TK assay and induction of apoptosis for compound 31 were investigated to assess its potential cytotoxic activity as a representative example of the novel synthesized compounds. At a concentration of 10 µM, compound 31 exhibited efficient inhibitory effect against EGFR-TK and induced apoptosis in MDA-MB-231 cells. Furthermore, a molecular docking study for compound 31 and erlotinib was performed to verify the binding mode toward the EGFR kinase enzyme, and showed a similar interaction as that with erlotinib alone. Graphical Abstract: Compound 31 showed potent antitumor activity and efficient inhibitory effect against EGFR-TK and induced apoptosis of MDA-MB-231 cells at a concentration of 10 µM.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Isatina/farmacologia
Simulação de Acoplamento Molecular
Quinazolinas/farmacologia
Receptor do Fator de Crescimento Epidérmico/antagonistas & inibidores
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Isatina/química
Estrutura Molecular
Quinazolinas/química
Receptor do Fator de Crescimento Epidérmico/metabolismo
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Quinazolines); 82X95S7M06 (Isatin); EC 2.7.10.1 (EGFR protein, human); EC 2.7.10.1 (Receptor, Epidermal Growth Factor)
[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:170719
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1344981


  8 / 771 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28646656
[Au] Autor:Xu Z; Song XF; Hu YQ; Qiang M; Lv ZS
[Ad] Endereço:Wuhan University of Science and Technology, 430081, Hubei, PR China.
[Ti] Título:Azide-alkyne cycloaddition towards 1H-1,2,3-triazole-tethered gatifloxacin and isatin conjugates: Design, synthesis and in vitro anti-mycobacterial evaluation.
[So] Source:Eur J Med Chem;138:66-71, 2017 Sep 29.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Twelve novel 1H-1,2,3-triazole-tethered gatifloxacin (GTFX) isatin conjugates 5a-l with greater lipophilicity compared with GTFX were designed, synthesized and evaluated for their in vitro anti-mycobacterial activities against M. tuberculosis (MTB) H Rv and MDR-TB as well as cytotoxicity. The preliminary results showed that all the targets (MIC: 0.10-8 µg/mL) exhibited excellent inhibitory activity against MTB H Rv and MDR-TB, but eight of them (CC : 7.8-62.5 µg/mL) were much more toxic than the parent GTFX (CC : 125 µg/mL). Among them, 5g (MIC: 0.10 µg/mL) was 4-8 times more potent in vitro than the references GTFX (MIC: 0.78 µg/mL) and RIF (MIC: 0.39 µg/mL) against MTB H Rv, but less active than INH (MIC: 0.05 µg/mL). The most potent 5g and 5h (MIC: 0.25 µg/mL) were 4->512 times more active than the three references (MIC: 1.0->128 µg/mL) against MDR-TB. Unfortunately, both of the two hybrids (CC : 7.8 µg/mL) were much more cytotoxic than the other derivatives, need to be further optimized.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Fluoroquinolonas/farmacologia
Isatina/farmacologia
Mycobacterium tuberculosis/efeitos dos fármacos
Triazóis/farmacologia
Tuberculose Resistente a Múltiplos Medicamentos/tratamento farmacológico
[Mh] Termos MeSH secundário: Alquinos/química
Alquinos/farmacologia
Animais
Antibacterianos/síntese química
Antibacterianos/química
Azidas/farmacologia
Sobrevivência Celular/efeitos dos fármacos
Cercopithecus aethiops
Reação de Cicloadição
Relação Dose-Resposta a Droga
Desenho de Drogas
Fluoroquinolonas/química
Isatina/química
Testes de Sensibilidade Microbiana
Estrutura Molecular
Relação Estrutura-Atividade
Triazóis/química
Células Vero
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkynes); 0 (Anti-Bacterial Agents); 0 (Azides); 0 (Fluoroquinolones); 0 (Triazoles); 82X95S7M06 (Isatin); L4618BD7KJ (gatifloxacin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170920
[Lr] Data última revisão:
170920
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170625
[St] Status:MEDLINE


  9 / 771 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28511906
[Au] Autor:Gao S; Zang J; Gao Q; Liang X; Ding Q; Li X; Xu W; Chou CJ; Zhang Y
[Ad] Endereço:Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Culture Road, 250012 Ji'nan, Shandong, PR China.
[Ti] Título:Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
[So] Source:Bioorg Med Chem;25(12):2981-2994, 2017 Jun 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:As a hot topic of epigenetic studies, histone deacetylases (HDACs) are related to lots of diseases, especially cancer. Further researches indicated that different HDAC isoforms played various roles in a wide range of tumor types. Herein a novel series of HDAC inhibitors with isatin-based caps and o-phenylenediamine-based zinc binding groups have been designed and synthesized through scaffold hopping strategy. Among these compounds, the most potent compound 9n exhibited similar if not better HDAC inhibition and antiproliferative activities against multiple tumor cell lines compared with the positive control entinostat (MS-275). Additionally, compared with MS-275 (IC values for HDAC1, 2 and 3 were 0.163, 0.396 and 0.605µM, respectively), compound 9n with IC values of 0.032, 0.256 and 0.311µM for HDAC1, 2 and 3 respectively, showed a moderate HDAC1 selectivity.
[Mh] Termos MeSH primário: Inibidores de Histona Desacetilases/química
Inibidores de Histona Desacetilases/farmacologia
Isatina/análogos & derivados
Isatina/farmacologia
Fenilenodiaminas/química
Fenilenodiaminas/farmacologia
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Desenho de Drogas
Histona Desacetilase 1/antagonistas & inibidores
Histona Desacetilase 1/química
Histona Desacetilase 1/metabolismo
Inibidores de Histona Desacetilases/síntese química
Seres Humanos
Isatina/síntese química
Simulação de Acoplamento Molecular
Neoplasias/tratamento farmacológico
Neoplasias/metabolismo
Neoplasias/patologia
Fenilenodiaminas/síntese química
Zinco/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histone Deacetylase Inhibitors); 0 (Phenylenediamines); 82X95S7M06 (Isatin); EC 3.5.1.98 (HDAC1 protein, human); EC 3.5.1.98 (Histone Deacetylase 1); J41CSQ7QDS (Zinc)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170801
[Lr] Data última revisão:
170801
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170518
[St] Status:MEDLINE


  10 / 771 MEDLINE  
              first record previous record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28425975
[Au] Autor:Xie Z; Wang G; Wang J; Chen M; Peng Y; Li L; Deng B; Chen S; Li W
[Ad] Endereço:College of Chemistry and Chemical Engineering, Hunan Engineering Laboratory for Analyse and Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou 416000, China. xiezz1993@126.com.
[Ti] Título:Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Isatin-Thiazole Derivatives as α-Glucosidase Inhibitors.
[So] Source:Molecules;22(4), 2017 Apr 20.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:A series of novel isatin-thiazole derivatives were synthesized and screened for their in vitro α-glucosidase inhibitory activity. These compounds displayed a varying degree of α-glucosidase inhibitory activity with IC ranging from 5.36 ± 0.13 to 35.76 ± 0.31 µm as compared to the standard drug acarbose (IC = 817.38 ± 6.27 µm). Among the series, compound bearing a hydroxyl group at the 4-position of the right phenyl and 2-fluorobenzyl substituent at the 1-positions of the 5-methylisatin displayed the highest inhibitory activity with an IC value of 5.36 ± 0.13 µm. Molecular docking studies revealed the existence of hydrophobic interaction, CH-π interaction, arene-anion interaction, arene-cation interaction, and hydrogen bond between these compounds and α-glucosidase enzyme.
[Mh] Termos MeSH primário: Inibidores de Glicosídeo Hidrolases/síntese química
Inibidores de Glicosídeo Hidrolases/farmacologia
Isatina/química
Simulação de Acoplamento Molecular
Tiazóis/química
alfa-Glucosidases/química
[Mh] Termos MeSH secundário: Sítios de Ligação
Simulação de Dinâmica Molecular
Estrutura Molecular
Ligação Proteica
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Glycoside Hydrolase Inhibitors); 0 (Thiazoles); 82X95S7M06 (Isatin); EC 3.2.1.20 (alpha-Glucosidases)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170531
[Lr] Data última revisão:
170531
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170421
[St] Status:MEDLINE



página 1 de 78 ir para página                         
   


Refinar a pesquisa
  Base de dados : MEDLINE Formulário avançado   

    Pesquisar no campo  
1  
2
3
 
           



Search engine: iAH v2.6 powered by WWWISIS

BIREME/OPAS/OMS - Centro Latino-Americano e do Caribe de Informação em Ciências da Saúde