Base de dados : MEDLINE
Pesquisa : D02.065.900 [Categoria DeCS]
Referências encontradas : 451 [refinar]
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[PMID]:28085281
[Au] Autor:Ravez S; Corbet C; Spillier Q; Dutu A; Robin AD; Mullarky E; Cantley LC; Feron O; Frédérick R
[Ad] Endereço:Medicinal Chemistry Research Group (CMFA), Louvain Drug Research Institute (LDRI), Université Catholique de Louvain , 73 avenue Mounier, B-1200 Brussels, Belgium.
[Ti] Título:α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).
[So] Source:J Med Chem;60(4):1591-1597, 2017 Feb 23.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Given the putative role of PHGDH in cancer, development of inhibitors is required to explore its function. In this context, we established and validated a straightforward enzymatic assay suitable for high-throughput screening and we identified inhibitors with similar chemical scaffolds. Through a convergent pharmacophore approach, we synthesized α-ketothioamides that exhibit interesting in vitro PHGDH inhibition and encouraging cellular results. These novel probes may be used to understand the emerging biology of this metabolic target.
[Mh] Termos MeSH primário: Inibidores Enzimáticos/química
Inibidores Enzimáticos/farmacologia
Fosfoglicerato Desidrogenase/antagonistas & inibidores
Tioamidas/química
Tioamidas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/química
Antineoplásicos/farmacologia
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Avaliação Pré-Clínica de Medicamentos
Ensaios de Triagem em Larga Escala
Seres Humanos
Neoplasias/tratamento farmacológico
Neoplasias/enzimologia
Fosfoglicerato Desidrogenase/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Enzyme Inhibitors); 0 (Thioamides); EC 1.1.1.95 (Phosphoglycerate Dehydrogenase)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170920
[Lr] Data última revisão:
170920
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170114
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.6b01166


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[PMID]:27795312
[Au] Autor:Gu W; Baral BS; DiSpirito AA; Semrau JD
[Ad] Endereço:Department of Civil and Environmental Engineering, University of Michigan, Ann Arbor, Michigan, USA.
[Ti] Título:An Aminotransferase Is Responsible for the Deamination of the N-Terminal Leucine and Required for Formation of Oxazolone Ring A in Methanobactin of Methylosinus trichosporium OB3b.
[So] Source:Appl Environ Microbiol;83(1), 2017 Jan 01.
[Is] ISSN:1098-5336
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Gene expression in methanotrophs has been shown to be affected by the availability of a variety of metals, most notably copper-regulating expression of alternative forms of methane monooxygenase. A copper-binding compound, or chalkophore, called methanobactin plays a key role in copper uptake in methanotrophs. Methanobactin is a ribosomally synthesized and posttranslationally modified peptide (RiPP) with two heterocyclic rings with an associated thioamide for each ring, formed from X-Cys dipeptide sequences that bind copper. The gene coding for the precursor polypeptide of methanobactin, mbnA, is part of a gene cluster, but the role of other genes in methanobactin biosynthesis is unclear. To begin to elucidate the function of these genes, we constructed an unmarked deletion of mbnABCMN in Methylosinus trichosporium OB3b and then homologously expressed mbnABCM using a broad-host-range cloning vector to determine the function of mbnN, annotated as coding for an aminotransferase. Methanobactin produced by this strain was found to be substantially different from wild-type methanobactin in that the C-terminal methionine was missing and only one of the two oxazolone rings was formed. Rather, in place of the N-terminal 3-methylbutanoyl-oxazolone-thioamide group, a leucine and a thioamide-containing glycine (Gly-Ψ) were found, indicating that MbnN is used for deamination of the N-terminal leucine of methanobactin and that this posttranslational modification is critical for closure of the N-terminal oxazolone ring in M. trichosporium OB3b. These studies provide new insights into methanobactin biosynthesis and also provide a platform for understanding the function of other genes in the methanobactin gene cluster. IMPORTANCE: Methanotrophs, microbes that play a critical role in the carbon cycle, are influenced by copper, with gene expression and enzyme activity changing as copper levels change. Methanotrophs produce a copper-binding compound, or chalkophore, called methanobactin for copper uptake, and methanobactin plays a key role in controlling methanotrophic activity. Methanobactin has also been shown to be effective in the treatment of Wilson disease, an autosomal recessive disorder where the human body cannot correctly assimilate copper. It is important to characterize the methanobactin biosynthesis pathway to understand how methanotrophs respond to their environment as well as to optimize the use of methanobactin for the treatment of copper-related diseases such as Wilson disease. Here we show that mbnN, encoding an aminotransferase, is involved in the deamination of the N-terminal leucine and necessary for the formation of one but not both of the heterocyclic rings in methanobactin that are responsible for copper binding.
[Mh] Termos MeSH primário: Imidazóis/química
Leucina/química
Methylosinus trichosporium/enzimologia
Oligopeptídeos/química
Oligopeptídeos/genética
Oxazolona/química
Transaminases/metabolismo
[Mh] Termos MeSH secundário: Cobre/metabolismo
Desaminação
Deleção de Genes
Expressão Gênica
Regulação Bacteriana da Expressão Gênica
Vetores Genéticos
Glicina/química
Glicina/metabolismo
Imidazóis/metabolismo
Leucina/metabolismo
Metionina/deficiência
Methylosinus trichosporium/genética
Methylosinus trichosporium/metabolismo
Família Multigênica
Oligopeptídeos/biossíntese
Oligopeptídeos/metabolismo
Oxazolona/metabolismo
Processamento de Proteína Pós-Traducional
Tioamidas/química
Tioamidas/metabolismo
Transaminases/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Imidazoles); 0 (Oligopeptides); 0 (Thioamides); 0 (methanobactin); 15646-46-5 (Oxazolone); 789U1901C5 (Copper); AE28F7PNPL (Methionine); EC 2.6.1.- (Transaminases); GMW67QNF9C (Leucine); TE7660XO1C (Glycine)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171102
[Lr] Data última revisão:
171102
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161101
[St] Status:MEDLINE


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[PMID]:27761972
[Au] Autor:Mukherjee S; Chatterjee J
[Ad] Endereço:Molecular Biophysics Unit, Indian Institute of Science, Bangalore, 560012, India.
[Ti] Título:Suppressing the epimerization of endothioamide peptides during Fmoc/t-Bu-based solid phase peptide synthesis.
[So] Source:J Pept Sci;22(11-12):664-672, 2016 Nov.
[Is] ISSN:1099-1387
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Despite a number of intriguing utilities associated with thioamide-containing peptides and proteins in the context of biophysics, pharmacology and chemical biology, it has hitherto remained as one of the underexplored territories of peptidomimetics. The synthesis of long mono to multiply substituted endothioamide peptides is invariably accompanied with severe epimerization, oxoamide formation and various other undesired side reactions, resulting in messy product profiles. This has completely restrained their use as novel chemical tools for biological studies. During the chain elongation of an N-terminally located thioamide peptide using the Fmoc/t-Bu chemistry, it becomes vulnerable to the repetitive basic treatments as required for such chemistry. The incompatibility of thioamide moiety with bases as well as strong coupling reagents leads to epimerization as well as other side reactions due to its nucleophilicity, resulting in the loss of the stereochemical identity of the thioamidated amino acid residue. An easy-to-implement and efficient protocol to synthesize long (>10-mer) endothioamide peptides, significantly suppressing epimerization and other side reactions using 10% piperidine/dimethylformamide for 1 min, is reported herein. The novelty of the protocol is shown through the efficient synthesis of a number of 10-12-mer mono to multiply thioamide-substituted peptides with broad substrate scopes. The utility of the protocol in the context of protein engineering and chemical protein synthesis is also shown through the synthesis of a thioamide version of the 16-mer peptide from the B1 domain of protein G. Such a protocol to synthesize long endothioamide peptides would open up avenues toward engineering and accessing novel thiopeptide and thioprotein-based chemical tools, the synthesis of which had been a serious hurdle thus far. Copyright © 2016 European Peptide Society and John Wiley & Sons, Ltd.
[Mh] Termos MeSH primário: Dimetilformamida/química
Fluorenos/química
Peptidomiméticos/síntese química
Piperidinas/química
Técnicas de Síntese em Fase Sólida/métodos
Tioamidas/química
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Proteínas de Bactérias/síntese química
Modelos Moleculares
Peptídeos/síntese química
Domínios Proteicos
Engenharia de Proteínas
Estrutura Secundária de Proteína
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bacterial Proteins); 0 (Fluorenes); 0 (IgG Fc-binding protein, Streptococcus); 0 (Peptides); 0 (Peptidomimetics); 0 (Piperidines); 0 (Thioamides); 67I85E138Y (piperidine); 8696NH0Y2X (Dimethylformamide)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170309
[Lr] Data última revisão:
170309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161021
[St] Status:MEDLINE
[do] DOI:10.1002/psc.2929


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[PMID]:27660182
[Au] Autor:Kucinska M; Piotrowska-Kempisty H; Lisiak N; Kaczmarek M; Dams-Kozlowska H; Granig WH; Höferl M; Jäger W; Zehl M; Murias M; Erker T
[Ad] Endereço:Department of Toxicology, Poznan University of Medical Sciences, Poznan, Poland.
[Ti] Título:Selective anticancer activity of the novel thiobenzanilide 63T against human lung adenocarcinoma cells.
[So] Source:Toxicol In Vitro;37:148-161, 2016 Dec.
[Is] ISSN:1879-3177
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Previously, it has been reported that molecules built on the benzanilide and thiobenzanilide scaffold are the promising groups of compounds with several biological activities including antifungal, antimycotic, antibacterial, spasmolytic, and anticancer ones. In this study the mechanism of action of one selected thiobenzanilide derivative N,N'-(1,2-phenylene)bis3,4,5-trifluorobenzothioamide (63T) with strongest cytotoxic activity has been investigated for the first time in human lung adenocarcinoma (A549) and normal lung derived fibroblast (CCD39Lu) in a cell culture model. The results demonstrated, that 63T can be considered a selective anticancer compound. Based on these results, several experiments including the analysis of cellular morphology, cell phase distribution, cytoplasmic histone-associated DNA fragmentation, apoptosis, necrosis, and autophagy detection were performed to understand better the mechanism underlying the anticancer activity. The data showed that 63T is a small molecule compound, which selectively induces cancer cell death in a caspase independent pathway; moreover, the autophagic dose-dependent processes may be involved in the mechanism of cell death.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Derivados de Benzeno/farmacologia
Tioamidas/farmacologia
[Mh] Termos MeSH secundário: Células A549
Adenocarcinoma
Apoptose/efeitos dos fármacos
Caspases/metabolismo
Ciclo Celular/efeitos dos fármacos
Linhagem Celular
Sobrevivência Celular/efeitos dos fármacos
Fragmentação do DNA
Seres Humanos
Neoplasias Pulmonares
Necrose/induzido quimicamente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Benzene Derivatives); 0 (N,N'-(1,2-phenylene)bis(3,4,5-trifluorobenzothioamide)); 0 (Thioamides); EC 3.4.22.- (Caspases)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170404
[Lr] Data última revisão:
170404
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160924
[St] Status:MEDLINE


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[PMID]:27548118
[Au] Autor:Abdelhamid AO; El Sayed IE; Hussein MZ; Mangoud MM
[Ad] Endereço:Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt. Abdelhamid45@gmail.com.
[Ti] Título:Synthesis and Antimicrobial Activity of Some New Thiadiazoles, Thioamides, 5-Arylazothiazoles and Pyrimido[4,5-d][1,2,4]triazolo[4,3-a]pyrimidines.
[So] Source:Molecules;21(8), 2016 Aug 17.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:A novel series of 1,3,4-thiadiazoles, 5-arylazothiazoles and hexahydropyrimido-[4,5-d][1,2,4]triazolo[4,3-a]pyrimidines were synthesized via reaction of hydrazonoyl halides with each of alkyl carbothioates, carbothioamides and 7-thioxo-5,6,7,8-tetrahydropyrimido-[4,5-d]pyrimidine-2,4(1H,3H)-diones in the presence of triethylamine. The structures of the newly synthesized compounds were established based on their spectral data, elemental analyses and alternative synthetic routes whenever possible. Also, the newly synthesized compounds were screened for their antimicrobial activity against various microorganisms.
[Mh] Termos MeSH primário: Anti-Infecciosos/síntese química
Pirimidinas/síntese química
Tiadiazóis/síntese química
Tioamidas/síntese química
[Mh] Termos MeSH secundário: Anti-Infecciosos/química
Anti-Infecciosos/farmacologia
Fungos/efeitos dos fármacos
Bactérias Gram-Negativas/efeitos dos fármacos
Bactérias Gram-Positivas/efeitos dos fármacos
Testes de Sensibilidade Microbiana
Estrutura Molecular
Pirimidinas/química
Pirimidinas/farmacologia
Tiadiazóis/química
Tiadiazóis/farmacologia
Tioamidas/química
Tioamidas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Pyrimidines); 0 (Thiadiazoles); 0 (Thioamides)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170414
[Lr] Data última revisão:
170414
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160823
[St] Status:MEDLINE


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[PMID]:27476140
[Au] Autor:Shin SY; Ahn S; Yoon H; Jung H; Jung Y; Koh D; Lee YH; Lim Y
[Ad] Endereço:Department of Biological Sciences, Konkuk University, Seoul 143-701, Republic of Korea.
[Ti] Título:Colorectal anticancer activities of polymethoxylated 3-naphthyl-5-phenylpyrazoline-carbothioamides.
[So] Source:Bioorg Med Chem Lett;26(17):4301-9, 2016 09 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:To develop potent chemotherapeutic agents for treating colorectal cancers, polymethoxylated 3-naphthyl-5-phenylpyrazoline-carbothioamide derivatives were designed. Twenty-two novel derivatives were synthesized and their cytotoxicities were measured using a clonogenic long-term survival assay. Of these derivatives, 3-(1-hydroxynaphthalen-2-yl)-N-(3-methoxyphenyl)-5-(4-methoxyphenyl)-pyrazoline-1-carbothioamide (NPC 15) exhibited the best half-maximal cell growth inhibitory concentrations (196.35nM). To explain its cytotoxicity, further biological experiments were performed. Treatment with NPC 15 inhibited cell cycle progression and triggered apoptosis through the caspase-mediated pathway. Its inhibitory effects on several kinases participating in the cell cycle were investigated using an in vitro kinase assay. Its half-maximal inhibitory concentrations for aurora kinases A and B were 105.03µM and 8.53µM, respectively. Further analysis showed that NPC 15 decreased phosphorylation of aurora kinases A, B, and C and phosphorylation of histone H3, a substrate of aurora kinases A and B. Its molecular binding mode for aurora kinase B was elucidated using in silico docking. In summary, polymethoxylated 3-naphthyl-5-phenylpyrazoline-carbothioamides could be potent chemotherapeutic agents.
[Mh] Termos MeSH primário: Neoplasias Colorretais/tratamento farmacológico
Tioamidas/farmacologia
[Mh] Termos MeSH secundário: Acetaldeído/análogos & derivados
Acetaldeído/química
Antineoplásicos/síntese química
Antineoplásicos/química
Antineoplásicos/farmacologia
Linhagem Celular
Sobrevivência Celular/efeitos dos fármacos
Seres Humanos
Simulação de Acoplamento Molecular
Naftóis/síntese química
Naftóis/química
Naftóis/farmacologia
Pirazóis/síntese química
Pirazóis/química
Pirazóis/farmacologia
Tioamidas/síntese química
Tioamidas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Naphthols); 0 (Pyrazoles); 0 (Thioamides); 29692-55-5 (naphthyl acetate); 5G4O7K64WA (2-methoxyacetaldehyde); GO1N1ZPR3B (Acetaldehyde)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171122
[Lr] Data última revisão:
171122
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160801
[St] Status:MEDLINE


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[PMID]:26813415
[Au] Autor:Hutton CA; Shang J; Wille U
[Ad] Endereço:School of Chemistry and Bio21 Institute, The University of Melbourne, 30 Flemington Road, Parkville, VIC, 3010, Australia. chutton@unimelb.edu.au.
[Ti] Título:Synthesis of Peptides by Silver-Promoted Coupling of Carboxylates and Thioamides: Mechanistic Insight from Computational Studies.
[So] Source:Chemistry;22(9):3163-9, 2016 Feb 24.
[Is] ISSN:1521-3765
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The mechanism of the recently described N→C direction peptide synthesis through silver-promoted coupling of N-protected amino acids with thioacetylated amino esters was explored by using density functional theory. Calculation of the potential energy surfaces for various pathways revealed that the reaction proceeds through silver-assisted addition of the carboxylate to the thioamide, which is followed by deprotonation and silver-mediated extrusion of sulfur as Ag2 S. The resulting isoimide is the key intermediate, which subsequently rearranges to an imide through a concerted pericyclic [1,3]-acyl shift (O-sp(2) N 1,3-acyl migration). The proposed mechanism clearly emphasises the requirement of two equivalents of Ag(I) and basic reaction conditions, which is in full agreement with the experimental findings. Alternative rearrangement pathways involving only one equivalent of Ag(I) or through O-sp(3) N 1,3-acyl migration can be excluded. The computations further revealed that peptide couplings involving thioformamides require significant conformational changes in the intermediate isoformimide, which slow down the rearrangement process.
[Mh] Termos MeSH primário: Ácidos Carboxílicos/química
Formamidas/química
Peptídeos/química
Prata/química
Compostos de Sulfidrila/química
Tioamidas/química
[Mh] Termos MeSH secundário: Estrutura Molecular
Teoria Quântica
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Carboxylic Acids); 0 (Formamides); 0 (Peptides); 0 (Sulfhydryl Compounds); 0 (Thioamides); 3M4G523W1G (Silver); G525TLN0E7 (thioformamide)
[Em] Mês de entrada:1607
[Cu] Atualização por classe:160215
[Lr] Data última revisão:
160215
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160128
[St] Status:MEDLINE
[do] DOI:10.1002/chem.201503753


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[PMID]:26799350
[Au] Autor:Prunty JJ; Heise CD; Chaffin DG
[Ad] Endereço:Department of Clinical Pharmacy, West Virginia University School of Pharmacy, Morgantown, West Virginia.
[Ti] Título:Graves' Disease Pharmacotherapy in Women of Reproductive Age.
[So] Source:Pharmacotherapy;36(1):64-83, 2016 Jan.
[Is] ISSN:1875-9114
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Graves' disease is an autoimmune disorder in which inappropriate stimulation of the thyroid gland results in unregulated secretion of thyroid hormones resulting in hyperthyroidism. Graves' disease is the most common cause of autoimmune hyperthyroidism during pregnancy. Treatment options for Graves' disease include thioamide therapy, partial or total thyroidectomy, and radioactive iodine. In this article, we review guideline recommendations for Graves' disease treatment in women of reproductive age including the recent guideline from the American College of Obstetricians and Gynecologists. Controversy regarding appropriate thioamide therapy before, during, and after pregnancy is reviewed. Surgical and radioactive iodine therapy considerations in this patient population are also reviewed. In patients who may find themselves pregnant during therapy or develop Graves' disease during their pregnancy, consideration should be given to the most appropriate treatment course for the mother and fetus. Thioamide therapy should be used with either propylthiouracil or methimazole at appropriate doses that target the upper range of normal to slightly hyperthyroid to avoid creating hypothyroidism in the fetus. Consideration should also be given to the adverse effects of thioamide, such as agranulocytosis and hepatotoxicity, with appropriate patient consultation regarding signs and symptoms. Individuals who wish to breastfeed their infants while taking thioamide should receive the lowest effective dose. Surgery should be reserved for extreme cases and limited to the second trimester, if possible. Radioactive iodine therapy may be used in nonpregnant individuals, with limited harm to future fertility. Radioactive iodine therapy should be withheld in pregnant women and those who are actively breastfeeding. Clinicians should keep abreast of developments in clinical trials and evidence-based recommendations regarding Graves' disease in reproductive-age women for any changes in evidence-based practice.
[Mh] Termos MeSH primário: Antitireóideos/uso terapêutico
Doença de Graves/tratamento farmacológico
[Mh] Termos MeSH secundário: Adulto
Antitireóideos/efeitos adversos
Feminino
Doença de Graves/complicações
Seres Humanos
Hipertireoidismo/complicações
Hipertireoidismo/tratamento farmacológico
Radioisótopos do Iodo/uso terapêutico
Gravidez
Complicações na Gravidez/tratamento farmacológico
Tioamidas/efeitos adversos
Tioamidas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antithyroid Agents); 0 (Iodine Radioisotopes); 0 (Thioamides)
[Em] Mês de entrada:1610
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160123
[St] Status:MEDLINE
[do] DOI:10.1002/phar.1676


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[PMID]:26745200
[Au] Autor:Shirinzadeh H; Ince E; Westwell AD; Gurer-Orhan H; Suzen S
[Ad] Endereço:a Department of Pharmaceutical Chemistry , Faculty of Pharmacy, Erzincan University , Yalnizbag Yerleskesi , Erzincan , Turkey .
[Ti] Título:Novel indole-based melatonin analogues substituted with triazole, thiadiazole and carbothioamides: studies on their antioxidant, chemopreventive and cytotoxic activities.
[So] Source:J Enzyme Inhib Med Chem;31(6):1312-21, 2016 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Melatonin (MLT) is a well-known free-radical scavenger, involving in the prevention of cellular damage that can lead to cancer, ageing and a variety of neurodegenerative diseases. Research on MLT-related compounds has been required to optimise the maximum pharmaceutical activity with the lowest side effects. In our ongoing research, we have synthesized new indole-based MLT analogues as potential antioxidant agents by modifying the MLT molecule. In this study, we build on previous findings, through the synthesis, characterization and in vitro antioxidant profiling of a series of new indole-based MLT analogues which possess triazole, thiadiazole and carbothioamides on the third position on the indole ring. In vitro antioxidant activity was investigated by evaluating their reducing effect against oxidation of a redox sensitive fluorescent probe and their radical scavenging activity was assessed via the DPPH assay. In addition, in vitro cytotoxic effects of newly synthesized compounds were investigated in CHO-K1 cells using the MTT assay.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Antioxidantes/farmacologia
Indóis/química
Melatonina/análogos & derivados
Tiadiazóis/química
Tioamidas/química
Triazóis/química
[Mh] Termos MeSH secundário: Animais
Células CHO
Espectroscopia de Ressonância Magnética Nuclear de Carbono-13
Quimioprevenção
Cricetinae
Cricetulus
Melatonina/química
Espectroscopia de Prótons por Ressonância Magnética
Espectrometria de Massas por Ionização por Electrospray
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Antioxidants); 0 (Indoles); 0 (Thiadiazoles); 0 (Thioamides); 0 (Triazoles); JL5DK93RCL (Melatonin)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170221
[Lr] Data última revisão:
170221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160109
[St] Status:MEDLINE
[do] DOI:10.3109/14756366.2015.1132209


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[PMID]:26730945
[Au] Autor:Kucinska M; Giron MD; Piotrowska H; Lisiak N; Granig WH; Lopez-Jaramillo FJ; Salto R; Murias M; Erker T
[Ad] Endereço:Department of Toxicology, Poznan University of Medical Sciences, Poznan, Poland.
[Ti] Título:Novel Promising Estrogenic Receptor Modulators: Cytotoxic and Estrogenic Activity of Benzanilides and Dithiobenzanilides.
[So] Source:PLoS One;11(1):e0145615, 2016.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The cytotoxicity of 27 benzanilides and dithiobenzanilides built on a stilbene scaffold and possessing various functional groups in aromatic rings previously described for their spasmolytic properties was assayed on three human cancer cell lines (A549 -lung adenocarcinoma, MCF-7 estrogen dependent breast adenocarcinoma and MDA-MB-231 estrogen independent breast adenocarcinoma) and 2 non-tumorigenic cell lines (CCD39Lu-lung fibroblasts, MCF-12A - breast epithelial). Three compounds (6, 15 and 18) showed selective antiproliferative activity against estrogen dependent MCF-7 cancer cells and their estrogenic activity was further confirmed in MCF-7 transfected with an estrogen receptor reporter plasmid and in HEK239 cells over-expressing the estrogen receptor alpha (ERα). Compound 18 is especially interesting as a potential candidate for therapy since it is highly toxic and selective towards estrogen dependent MCF7 cell lines (IC50 = 5.07 µM versus more than 100 µM for MDA-MB-231) and almost innocuous for normal breast cells (IC50 = 91.46 µM for MCF-12A). Docking studies have shown that compound 18 interacts with the receptor in the same cavity as estradiol although the extra aromatic ring is involved in additional binding interactions with residue W383. The role of W383 and the extended binding mode were confirmed by site-directed mutagenesis.
[Mh] Termos MeSH primário: Anilidas/farmacologia
Proliferação Celular/efeitos dos fármacos
Moduladores de Receptor Estrogênico/farmacologia
Tioamidas/farmacologia
[Mh] Termos MeSH secundário: Anilidas/química
Anilidas/metabolismo
Sítios de Ligação/genética
Linhagem Celular
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Estradiol/química
Estradiol/metabolismo
Estradiol/farmacologia
Moduladores de Receptor Estrogênico/química
Moduladores de Receptor Estrogênico/metabolismo
Estrogênios/química
Estrogênios/metabolismo
Estrogênios/farmacologia
Células HEK293
Seres Humanos
Células MCF-7
Modelos Moleculares
Estrutura Molecular
Mutação
Ligação Proteica
Estrutura Terciária de Proteína
Receptores Estrogênicos/química
Receptores Estrogênicos/genética
Receptores Estrogênicos/metabolismo
Tioamidas/química
Tioamidas/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anilides); 0 (Estrogen Receptor Modulators); 0 (Estrogens); 0 (Receptors, Estrogen); 0 (Thioamides); 4TI98Z838E (Estradiol); AK1B12366O (benzanilide)
[Em] Mês de entrada:1607
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160106
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0145615



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