Search results for "TIMIT"

showing 10 items of 150 documents

Heterocyclic and Phenyl Double-Bond-Locked Combretastatin Analogues Possessing Potent Apoptosis-inducing activity in HL60 and in MDR Cell lines

2005

Two new series of combretastatin (CA-4) analogues have been prepared. The alkenyl motif of CA-4 was replaced either by a five-membered heterocyclic (isoxazoline or isoxazole) or by a six-membered ring (pyridine or benzene). The new compounds have been evaluated for their effects on tubulin assembly and for cytotoxic and apoptotic activities. Five compounds (18b, 20a, 21a, 34b, and 35b) demonstrated an attractive profile of cytotoxicity (IC501 microM) and apoptosis-inducing activity but poor antitubulin activity. The isoxazoline derivatives 18b, 20a, and 21a, demonstrated potent apoptotic activity different from that of natural CA-4. Their ability to block most cells in the G2 phase suggests…

Models MolecularA-4 ANALOGSDouble bondHL60StereochemistryPyridinesTUBULINApoptosisANTINEOPLASTIC AGENTSchemistry.chemical_compoundStructure-Activity RelationshipCell Line TumorDrug DiscoveryStilbenesBenzene DerivativesHumansIsoxazoleBIOLOGICAL EVALUATIONCytotoxicitychemistry.chemical_classificationCombretastatinbiologyCOLCHICINEDEATHIsoxazolesDrug Resistance MultipleTubulinANTIMITOTIC ANTITUMOR AGENTSMULTIDRUGchemistryApoptosisCell cultureDrug Resistance NeoplasmDISCOVERYbiology.proteinMolecular MedicineDrug Screening Assays AntitumorSOLID TUMOR-THERAPY
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Synthesis and Biological Evaluation of 1-Methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a New Class of Antimitotic Agents and Tubulin Inhibi…

2008

The 2-(3,4,5-trimethoxybenzoyl)-2-aminoindole nucleus was used as the fundamental structure for the synthesis of compounds modified with respect to positions C-4 to C-7 with different moieties (chloro, methyl, or methoxy). Additional structural variations concerned the indole nitrogen, which was alkylated with small alkyl groups such as methyl or ethyl. We have identified 1-methyl-2-(3,4,5-trimethoxybenzoyl)-3-amino-7-methoxyindole as a new highly potent antiproliferative agent that targets tubulin at the colchicine binding site and leads to apoptotic cell death.

Models MolecularIndolesStereochemistryAlkylationAntimitotic AgentsChemical synthesisMiceStructure-Activity RelationshipBiopolymersTubulinCell Line TumorDrug DiscoveryStructure–activity relationshipAnimalsHumansIndole testBinding SitesbiologyTubulin ModulatorsChemistryBiological activityTubulin ModulatorsTubulinbiology.proteinMolecular MedicineAntimitotic AgentDrug Screening Assays AntitumorColchicineProtein Binding
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NGO Legitimacy as a Continuous Negotiation Process : Fostering ‘Good Citizenship’ in Western Uganda

2022

The article draws on and contributes to debates on the legitimacy of non-governmental organizations (NGOs) engaged in development, defining organizational legitimacy as a social construct that is continually negotiated in relationships with diverse audiences. To explore the negotiated nature of NGO legitimacy, the article examines the efforts of a Ugandan NGO, Kabarole Research and Resource Centre (KRC), to foster citizens’ capacities in rural communities in the western part of the country. Drawing on interviews and participant observation, we scrutinize the ways in which KRC balances between different and even contrasting legitimacy expectations stemming from three types of encounters sign…

NGOsafrikkalaisuuskehitysyhteistyöcivic educationUgandalegitimiteettikansalaisuusneuvottelutyhteisötkansalaistoimintakehitystutkimuskansalaisjärjestöt
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Deformable object segmentation in ultra-sound images

2013

Breast cancer is the second most common type of cancer being the leading cause of cancer death among females both in western and in economically developing countries. Medical imaging is key for early detection, diagnosis and treatment follow-up. Despite Digital Mammography (DM) remains the reference imaging modality, Ultra-Sound (US) imaging has proven to be a successful adjunct image modality for breast cancer screening, specially as a consequence of the discriminative capabilities that US offers for differentiating between solid lesions that are benign or malignant. Despite US usability,US suffers inconveniences due to its natural noise that compromises the diagnosis capabilities of radio…

OptimizationUltrasonore62Tesis i dissertacions acadèmiquesBag-of-wordsOptimization frameworkComputingMethodologies_IMAGEPROCESSINGANDCOMPUTERVISIONOptimizaciónCàncer de mamaBreast cancerSegmentationCáncer de mamaMachine learning616UltrasoundOptimitzacióFeatures[SPI.SIGNAL] Engineering Sciences [physics]/Signal and Image processingUltrasòSegmentaciónSegmentació[SDV.IB.IMA] Life Sciences [q-bio]/Bioengineering/ImagingComputingMethodologies_PATTERNRECOGNITIONUltrasonidoBag-of-features616 - Patologia. Medicina clínica. OncologiaGraph-cutsMedical imaging62 - Enginyeria. Tecnologia
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EMPATIA E BISOGNO DI DIGNITA' DELLA PERSONA

2013

In questo saggio viene approfondito il senso dell'empatia come primo esistenziale, muovendosi nella prospettiva di un'antropologia pedagogica del bisogno fondamentale di riconoscimento. Si tratta, in quanto costituisce il lato affettivo del riconoscimento, di un bisogno di essere accolti, grazie ad un accudimento empatico, nella nostra singolarità; è la ragione per cui si può chiamare bisogno d’intimità. In quello che invece costituisce il lato culturale ed etico, si tratta del bisogno di essere introdotti, grazie ad un dialogo centrato sull’empatia, in un universo simbolico. Poiché ci accompagna la certezza che vivere nella ricerca del senso e testimoniando questa ricerca valga di più che …

Primo esistenziale bisogno di riconoscimento antropologia pedagogica bisogno di intimità bisogno di dignità.Settore M-PED/01 - Pedagogia Generale E Sociale
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Bērnu atveidojums sociālajos tīklos "Facebook.com" un "draugiem.lv"

2017

Bakalaura darba tēma ir “Bērnu atveidojums sociālajos tīklos facebook.com un draugiem.lv”. Darbs galvenokārt sastāv no lietotāju profilu saturu pētījuma analīzes, kur ir redzams vai pieminēts bērns. Publicētie ieraksti atlasīti laika periodā no 2014. gada 1. aprīļa līdz 2016. gada 31. decembrim. Bakalaura darba izvirzītais pētnieciskais jautājums–cik daudzpusīgi bērnu vecāki sociālajos tīklos nodod privātu un precīzu informāciju par saviem bērniem, pakļaujot riskam bērna drošību un privātumu. Darba teorētiskajā daļā raksturoti sociālie tīkli, to specifika,definēts intimitātes,privātuma un ievainojamības jēdziens, socializācija un sevisizrādīšana sabiedrībā, kā arī apskatīts bērnu normatīvo …

PrivātumsIntimitātesociālie tīkliSocializācijaKomunikācijas zinātnebērns
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Cytotoxicity and antimitotic activity of Rhinella schneideri and Rhinella marina venoms.

2019

Abstract Ethnopharmacological relevance Rhinella schneideri and Rhinella marina are toad venoms distributed in different parts of the world, including Brazil, Columbia and amazon. Venoms extracted from different species have many clinical applications such as antimicrobial cardiotonics and treatment of cancer. Aim of the study; In this study, we aim to investigate the effect of venoms extracted from R. schneideri and R. marina on cancer cells and verify possible mechanism of action. Material and method Cytotoxicity analyses was performed using the resazurin reduction assay, where different concentrations of venoms were tested against sensitive CCRF-CEM and P-gp overexpressing ADR/CEM5000 le…

Programmed cell deathCell SurvivalAntimitotic AgentsLethal Dose 5003 medical and health scienceschemistry.chemical_compound0302 clinical medicineTubulinRhinella schneideriCell Line TumorDrug DiscoveryAnimalsHumansPropidium iodideCytotoxicity030304 developmental biologyPharmacology0303 health sciencesbiologyBufalinCell Cycle Checkpointsbiology.organism_classificationBufonidaeMolecular Docking SimulationTubulinchemistryBiochemistryApoptosis030220 oncology & carcinogenesisCancer cellbiology.proteinAmphibian VenomsJournal of ethnopharmacology
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Synthesis of a new class of pyrrolo[3,4-h]quinazolines with antimitotic activity

2014

Abstract A new series of pyrrolo[3,4- h ]quinazolines was conveniently prepared with a broad substitution pattern. A large number of derivatives was obtained and the cellular cytotoxicity was evaluated in vitro against 5 different human tumor cell lines with GI 50 values reaching the low micromolar level (1.3–19.8 μM). These compounds were able to induce cell death mainly by apoptosis through a mitochondrial dependent pathway. Selected compounds showed antimitotic activity and a reduction of tubulin polymerization in a concentration-dependent manner. Moreover, they showed anti-angiogenic properties since reduced in vitro endothelial cell migration and disrupted HUVEC capillary-like tube net…

Programmed cell deathMitosisAntiproliferative activityCell Line TumorDrug DiscoveryHuman Umbilical Vein Endothelial CellsPiHumansTubulin polymerizationPyrrolesPyrrolo[3Cell-mediated cytotoxicityPyrrolo[34-h]quinazolines Antiproliferative activity Antimitotic activity Tubulin polymerization Vascular disrupting activityTubulin polymerizationVascular disrupting activityPharmacologyMatrigelCell Death4-h]quinazolinesChemistryAntimitotic activityOrganic ChemistryGeneral MedicineSettore CHIM/08 - Chimica FarmaceuticaMitochondriaEndothelial stem cellBiochemistryCell cultureApoptosisPyrrolo[3; 4-h]quinazolines; Antiproliferative activity; Antimitotic activity; Tubulin polymerization; Vascular disrupting activityQuinazolinesLysosomes
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Power of Paradox: Grassroots Organizations’ Legitimacy Strategies Over Time

2021

Fringe stakeholders with limited resources, such as grassroots organizations (GROs), are often ignored in business and society literature. We develop a conceptual framework and a set of propositions detailing how GROs strategically gain legitimacy and influence over time. We argue that GROs encounter specific paradoxes over the emergence, development, and resolution of an issue, and they address these paradoxes using cognitive, moral, and pragmatic legitimacy strategies. While cognitive and moral strategies tend to be used consistently, the flexible and paradoxical use of pragmatic strategies has important consequences, both for GROs’ legitimacy and for their potential influence over powerf…

PropositionPublic administration0603 philosophy ethics and religionSocial activismPower (social and political)GrassrootsPolitical science0502 economics and businessissues managementSet (psychology)Legitimacy05 social sciences06 humanities and the artsstakeholder influencesosiaalinen oikeudenmukaisuusstrategiatConceptual frameworkBusiness Management and Accounting (miscellaneous)legitimiteetti060301 applied ethicsaktivismiLimited resourcessocial activismkansalaistoiminta050203 business & managementSocial Sciences (miscellaneous)Business & Society
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Synthesis and Biological Evaluation of 2-Amino-3-(3’,4’,5’-Trimethoxybenzoyl)-6-Substituted-4,5,6,7-Tetrahydrothieno[2,3-c]pyridine Derivatives as An…

2008

Microtubules are among the most successful targets of compounds potentially useful for cancer therapy. A new series of inhibitors of tubulin polymerization based on the 2-amino-3-(3,4,5-trimethoxybenzoyl)-4,5,6,7-tetrahydrothieno[b]pyridine molecular skeleton was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. The most promising compound in this series was 2-amino-3-(3,4,5-trimethoxybenzoyl)-6-methoxycarbonyl-4,5,6,7-tetrahydrothieno[b]pyridine, which inhibits cancer cell growth with IC(50)-values ranging from 25 to 90 nM against a panel of four cancer cell lines, and interacts strongly with tubulin by binding to the co…

PyridinesStereochemistryClinical BiochemistryPharmaceutical ScienceAntimitotic AgentsCrystallography X-RayBiochemistryChemical synthesisArticleInhibitory Concentration 50Structure-Activity Relationshipchemistry.chemical_compoundTubulinMicrotubuleDrug DiscoveryPyridineAnimalsStructure–activity relationshipCytotoxicityMolecular BiologyMolecular StructurebiologyBicyclic moleculeChemistryOrganic ChemistryTubulinbiology.proteinMolecular MedicineAntimitotic Agent
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