Search results for "I.5"
showing 10 items of 399 documents
Immunoreagents and competitive assays to fludioxonil
2014
Fludioxonil is a new-generation fungicide widely used for postharvest fruit protection. The aim of this study was to produce hitherto unreported immunoreagents for Fludioxonil analysis by immunoassay. Derivatives of this agrochemical were synthesized with different linker tethering sites. Those functionalized haptens were activated, and the purified active esters were efficiently conjugated to different carrier proteins for immunogen and assay antigen preparation. Antibodies to Fludioxonil were raised in rabbits, and their selectivity and affinity were characterized, revealing the significance of the linker. Those antibodies were evaluated using homologous and heterologous conjugates by dir…
Synthesis and Antiproliferative Activity of Novel 3-(Indazol-3-yl)-quinazolin-4(3H)-one and 3-(Indazol-3-yl)-benzotriazin-4(3H)-one Derivatives
1999
Several new 3-(indazol-3-yl)-quinazolin-4(3H)-one and 3-(indazol-3-yl)-benzotriazin-4(3H)-one derivatives 5 and 6 were synthesized and tested for their in vitro antiproliferative activity against Raji, K562, and K562-R cell lines. The pharmacological screening showed that some 2, 6, or 7-substituted quinazolinones 5 posses a significant antiproliferative activity, with a percentage growth inhibition ranging from 44.8% to 100% at 50 microM, which was higher than that showed by the unsubstituted derivative 5a previously synthesized. For the most active compounds 5d, 5f, and 5g the IC50 were recorded.
SYNTHESIS AND PHOTOCHEMIOTHERAPEUTIC ACTIVITY OF THIOPYRANO[2,3-E]INDOL-2-ONES
2004
A series of derivatives of the new ring system thiopyrano[2,3-e]indol-2-one was prepared with the aim of obtaining new photochemotherapeutic drugs. Biological screenings were performed on this new class of photoactivable drugs and a strong antiproliferative effect was observed upon irradiation with UVA light. The compound bearing a methyl substituent at the pyrrole nitrogen resulted as the most interesting showing IC50 in the nanomolar range.
Imidazo[2,1-b] [1,3,4]thiadiazoles with antiproliferative activity against primary and gemcitabine-resistant pancreatic cancer cells
2020
A new series of eighteen imidazo [2,1-b] [1,3,4]thiadiazole derivatives was efficiently synthesized and screened for antiproliferative activity against the National Cancer Institute (NCI-60) cell lines panel. Two out of eighteen derivatives, compounds 12a and 12h, showed remarkably cytotoxic activity with the half maximal inhibitory concentration values (IC50) ranging from 0.23 to 11.4 μM, and 0.29–12.2 μM, respectively. However, two additional compounds, 12b and 13g, displayed remarkable in vitro antiproliferative activity against pancreatic ductal adenocarcinoma (PDAC) cell lines, including immortalized (SUIT-2, Capan-1, Panc-1), primary (PDAC-3) and gemcitabine-resistant (Panc-1R), elici…
A novel target of lithium therapy.
2000
Phosphatases converting 3'-phosphoadenosine 5'-phosphate (PAP) into adenosine 5'-phosphate are of fundamental importance in living cells as the accumulation of PAP is toxic to several cellular systems. These enzymes are lithium-sensitive and we have characterized a human PAP phosphatase as a potential target of lithium therapy. A cDNA encoding a human enzyme was identified by data base screening, expressed in Escherichia coli and the 33 kDa protein purified to homogeneity. The enzyme exhibits high affinity for PAP (K(m)1 microM) and is sensitive to subtherapeutic concentrations of lithium (IC(50)=0.3 mM). The human enzyme also hydrolyzes inositol-1, 4-bisphosphate with high affinity (K(m)=0…
Uzvedības paradumu veicināšana 5-6 gadu veciem bērniem pirmsskolas izglītības iestādēs dienas ritā
2022
Kvalifikācijas darba temats ir „Uzvedības paradumu veicināšana 5-6 gadus veciem bērniem pirmsskolas izglītības iestādes dienas ritā”. Kvalifikācijas darba autore ir Diāna Stepuļonoka. Pētījuma mērķis - pētīt 5-6 gadus vecu bērnu uzvedības paradumus pirmsskolas iestādes dienas ritā. Teorētiskajā daļā autore analizēja literatūru par 5-6 gadus vecu bērnu uzvedības paradumiem un pirmsskolas izglītības iestādēs dienas ritu. Empirīskajā daļā autore veica pētījumu pirmsskolas izglītības iestādē dienas rītā par bērnu uzvedības paradumu izmaiņām un analizēja to. Pētījuma rezultātā autore secināja, ka 5-6 gadu vecu bērnu pieklājīgas uzvedības paradumi tiek veicināti, ja: skolotājs nodrošina saturu bē…
Job Satisfaction among Primary School Personnel
2016
International audience; This article analyzes the job satisfaction of primary school teachers inMadagascar. Based on the estimation of multilevel models, low wages and problems getting paid, job insecurity, lack of in-service training, high pupil-teacher ratios, and lack of basic infrastructure and teaching materials are identified as the main reasons for dissatisfaction. Principals' control of teachers' activities also adversely affects satisfaction, suggesting that, in Malagasy schools, neither school directors nor teachers have succeeded in adopting organizational cultures based on cooperation among their members. These results are likely to stimulate debates on educational policy, both …
Landscapes of loss and destruction: : Sámi elders’ childhood memories of the second world war
2019
The so-called Lapland War between Finland and Germany at the end of the Second World War led to a mass-scale destruction of Lapland. Both local Finnish residents and the indigenous Sámi groups lost their homes, and their livelihoods suffered in many ways. The narratives of these deeply traumatic experiences have long been neglected and suppressed in Finland and have been studied only recently by academics and acknowledged in public. In this text, we analyze the interviews with four elders of one Sámi village, Vuotso. We explore their memories, from a child’s perspective, scrutinizing the narration as a multilayered affective process that involves sensual and embodied dimensions of memory. ©…
Students’ Interpretations of a Persuasive Multimodal Video About Vaccines
2021
The present study investigated students’ (N = 404) interpretations of the main message and use of modes in a persuasive multimodal video on vaccines. It also examined whether students’ topic knowledge, language arts grades, and self-identified gender were associated with their interpretations. Students analyzed a YouTube video in which two entertainers demonstrated the importance of vaccinating children. Students’ interpretations of the usefulness of vaccines varied in terms of quality of reasoning, which was associated with students’ topic knowledge. Notably, many students’ interpretations of the use of modes were incomplete, or they did not even mention certain modes in their response. Th…
Crystal Structures and Cytotoxicity of ent-Kaurane-Type Diterpenoids from Two Aspilia Species
2018
A phytochemical investigation of the roots of Aspilia pluriseta led to the isolation of ent-kaurane-type diterpenoids and additional phytochemicals (1⁻23). The structures of the isolated compounds were elucidated based on Nuclear Magnetic Resonance (NMR) spectroscopic and mass spectrometric analyses. The absolute configurations of seven of the ent-kaurane-type diterpenoids (3⁻6, 6b, 7 and 8) were determined by single crystal X-ray diffraction studies. Eleven of the compounds were also isolated from the roots and the aerial parts of Aspilia mossambicensis. The literature NMR assignments for compounds 1 and 5 were revised. In a cytotoxicity assay, 12α-methoxy-ent-kaur-9(11),1…