Search results for "LOGS"
showing 10 items of 229 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…
1,2,4-Oxadiazole Topsentin Analogs with Antiproliferative Activity against Pancreatic Cancer Cells, Targeting GSK3β Kinase.
2021
A new series of topsentin analogs, in which the central imidazole ring of the natural lead was replaced by a 1,2,4- oxadiazole moiety, was efficiently synthesized. All derivatives were pre-screened for antiproliferative activity against the National Cancer Institute (NCI-60) cell lines panel. The five most potent compounds were further investigated in various pancreatic ductal adenocarcinoma (PDAC) cell lines, including SUIT-2, Capan-1, and Panc-1 cells, eliciting EC50 values in the micromolar and sub-micromolar range, associated with significant reduction of cell migration. These remarkable results might be explained by the effects of these new topsentin analogues on epithelial-to-mesenchy…
Phosphonic Acid Analogs of Fluorophenylalanines as Inhibitors of Human and Porcine Aminopeptidases N: Validation of the Importance of the Substitutio…
2020
International audience; A library of phosphonic acid analogs of phenylalanine substituted with fluorine, chlorine and trifluoromethyl moieties on the aromatic ring was synthesized and evaluated for inhibitory activity against human (hAPN) and porcine (pAPN) aminopeptidases. Fluorogenic screening indicated that these analogs are micromolar or submicromolar inhibitors, both enzymes being more active against hAPN. In order to better understand the mode of the action of the most active compounds, molecular modeling was used. It confirmed that aminophosphonic portion of the enzyme is bound nearly identically in the case of all the studied compounds, whereas the difference in activity results fro…
Vidējā pirmsskolas vecuma bērnu monologa runas prasmju pilnveide radošajās rotaļās
2017
Bakalaura darba autors: Linda Kruglauža Bakalaura darba vadītājs: profesore, Dr. paed. Maruta Sīle Bakalaura darba temats: “Vidējā pirmsskolas vecuma bērnu monologa runas prasmju pilnveide radošajās rotaļās”. Pētījuma mērķis: Pētīt vidējā pirmsskolas vecuma bērnu monologa runas prasmju pilnveides iespējas radošajās rotaļās Darbs sastāv no 2 daļām – teorētiskās un empīriskās. Teorētiskajā daļā, balstoties uz zinātnieku atziņām, tika veikta analīze par monologa runas jēdzienu. Darba otrajā, empīriskajā daļā, lai būtu iespējams izvērtēt kvantitatīvi bērnu monologa runas prasmju pilnveidi radošajās rotaļās tika izstrādāti 4 kritēriji, katram no tiem 2 rādītāji. Kopumā, izvērtējot sasniegtos rez…
Modes katalogu dizaina vizuālā stilistika
2020
Latvijas Universitātes Pedagoģijas, psiholoģijas un mākslas fakultātes Datorgrafikas nodaļas Mākslas profesionālā bakalaura studiju programmas 4. kursa studentes Lauras Anspokas (Stud. apl. Nr. la16037) diplomdarbā „Modes katalogu vizuālā stilistika” tiek pētīta modes katalogu pielietojamība un attīstības tendences mūsdienās, kā arī Latvijas dizaineru radītās modes skatāmgrāmatas jeb katalogi. Diplomdarbā ir trīs daļas. Teorētiskajā daļā tiek apkopota informācija par modes katalogu vēsturi, to attīstības gaitu līdz mūsdienām, modes katalogu veidiem. Empīriskajā daļā tiek apskatītas un analizētas mūsdienu Latvijas dizaineru radītās modes skatāmgrāmatas un katalogi pēc četriem autores izveido…
A computational study to explore the molecular mechanisms behind the antiproliferative activity of Nortopsentin derivatives
2018
Lenalidomide Maintenance After Autologous Stem-Cell Transplantation in Newly Diagnosed Multiple Myeloma: A Meta-Analysis
2017
Purpose Lenalidomide maintenance therapy after autologous stem-cell transplantation (ASCT) demonstrated prolonged progression-free survival (PFS) versus placebo or observation in several randomized controlled trials (RCTs) of patients with newly diagnosed multiple myeloma (NDMM). All studies had PFS as the primary end point, and none were powered for overall survival (OS) as a primary end point. Thus, a meta-analysis was conducted to better understand the impact of lenalidomide maintenance in this setting. Patients and Methods The meta-analysis was conducted using primary-source patient-level data and documentation from three RCTs (Cancer and Leukemia Group B 100104, Gruppo Italiano Malatti…
Cetuximab rechallenge in metastatic colorectal cancer patients: how to come away from acquired resistance?
2012
Background: Scientific data provide the evidence that secondary K-RAS mutations do not occur during anti-epidermal growth factor receptor therapy in colorectal cancer patients. This multicenter phase II prospective study aims to investigate the activity of a retreatment with a cetuximab-based therapy. Patients and methods: We enrolled 39 irinotecan-refractory patients who had a clinical benefit after a line of cetuximab- plus irinotecan-based therapy and then a progression of disease for which underwent a new line chemotherapy and finally, after a clear new progression of disease, were retreated with the same cetuximab- plus irinotecan-based therapy. Results: Median number of therapeutic li…
Safety of the first dose of fingolimod for multiple sclerosis: results of an open-label clinical trial
2014
BACKGROUND: In patients with relapsing-remitting MS (RRMS) fingolimod prevents disease relapses and delays disability progression. First dose administration of fingolimod is associated with a transient, dose-dependent decrease in heart rate (HR) in the 6 hours after drug intake.The aim of the study is to to assess safety and tolerability of the first dose of fingolimod in a cohort of Italian patients with RRMS without alternative therapeutic options. METHODS: Open-label, single arm, multicentre study. After the first dose of fingolimod, patients were observed for 6 hours and had their vital signs monitored hourly. Extended on-site monitoring was provided when required. RESULTS: Of the 906 p…
Muzeja pamatkrājuma elektroniskais katalogs
2019
Kvalifikācijas darbā ir izstrādāts Latvijas Universitātes muzeja pamatkrājuma elektroniskais katalogs. Sākotnēji, muzeja darbinieki muzeja eksponenta uzskaiti veidoja excel formātā, kur bija apkopoti dati par priekšmetu autoriem, izmēriem, topogrāfijas novietojumiem utt.. Tomēr šie dokumenti bija tikai redzami muzeja darbiniekiem, un nebija saskarsmes ar lietotāju. Tādēļ tika nolemts, ka nepieciešams datus konvertēt uz jaunu datubāzi, kurai tiek veidota lietotāju saskarsme caur Latvijas Universitāti. Pēc sistēmu ievades, lietotāji varēs apskatīt kuri priekšmeti un kurā vietā no katra muzeja kataloga ir izlikti kā eksponenti, savukārt muzeja darbinieki ir vienīgie kuri varēs rediģēt vai piev…