Search results for "activity"

Pyrido[2’,3’:4,5]pyrrolo[2,1-d][1,2,3,5]tetrazine-4(3H)-ones, a new class of temozolomide heteroanalogues

2009

Twelve derivatives of new ring system pyrido[2’,3’:4,5]pyrrolo[2,1-d][1,2,3,5]tetrazine were prepared in good yields by reaction of 2-diazo-3-ethoxycarbonyl-pyrrolo[3,2-b]pyridine with alkyl- or aryl-isocyanates. Nine derivatives, screened by the National Cancer Institute (Bethesda, MD) for the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity.

SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF 3-AMINO-N-PHENYL-1H-INDAZOLE-1-CARBOXAMIDES

2010

Recently our research group has reported the synthesis of some 3-amino-N-phenyl-1H-indazole-1-carboxamides able to inhibit at low micromolar concentrations the cell growth of many neoplastic cell lines. The above compounds are unsubstituted in the indazole nucleus and this gives the hope to obtain more active compounds if appropriate substituents are beared by the above nucleus. So, several new N-phenyl-1H-indazole-1-carboxamides 1c-h and 4l,m were prepared by reacting phenyl isocyanates 3a,b with 3-amino-1H-indazoles 2c,e,g, or 1H-indazole 2l respectively. Chemical trasformations of compounds 1a,b and 1g,h gave 3-acetamido-N-phenyl-1H-indazole-1-carboxamides 5a,b, and 3,5-diamino-N-phenyl-…

Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality.

2015

Several new 2-(2-phenoxyacetamido)benzamides 17a-v, 21 and 22 were synthesized by stirring in pyridine the acid chlorides 16a-e and the appropriate5-R-4-R1-2-aminobenzamide 15a-e and initially evaluated in vitro for antiproliferative activity against the K562 (human chronic myelogenous leukemia) cell line. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). The most active compounds caused an arrest of K562 cells in the G0-G1 phase of cell cycle and induction of apoptos…

Rethinking children’s physical activity interventions at school: A new context-specific approach

2023

Physical activity is important for children’s health. However, evidence suggests that many children and adults do not meet international physical activity recommendations. Current school-based interventions have had limited effect on physical activity and alternative approaches are needed. Context, which includes school setting, ethos, staff, and sociodemographic factors, is a key and largely ignored contributing factor to school-based physical activity intervention effectiveness, impacting in several interacting ways.ConceptualizationCurrent programs focus on tightly-constructed content that ignores the context in which the program will be delivered, thereby limiting effectiveness. We prop…

A dual process model to predict adolescents’ screen time and physical activity

2021

OBJECTIVE: Many adolescents report a lack of physical activity (PA) and excess screen time (ST). Psychological theories aiming to understand these behaviours typically focus on predictors of only one behaviour. Yet, behaviour enactment is often a choice between options. This study sought to examine predictors of PA and ST in a single model. Variables were drawn from dual process models, which portray behaviour as the outcome of deliberative and automatic processes. DESIGN: 411 Finnish vocational school students (age 17-19) completed a survey, comprising variables from the Reasoned Action Approach (RAA) and automaticity pertaining to PA and ST, and self-reported PA and ST four weeks later. M…

Endohedral Mixed Aggregates: Sodium Alkoxide Cages with Organic or Inorganic Central Anions and Variable Hull.

2021

Abstract Alkali metal alkoxides are widely used in chemistry due to their Brønsted basic and nucleophilic properties. Potassium alkoxides assist alkyllithium in the metalation of hydrocarbons in Lochmann‐Schlosser‐bases. Both compounds form mixed aggregates, which enhance the thermal stability, solubility, and the basic reactivity of these mixtures. A very unusual spherical mixed alkoxy aggregate was discovered by Grützmacher et al., where a central dihydrogen phosphide anion is surrounded by a highly dynamic shell of thirteen sodium atoms and a hull of twelve tert‐butoxide groups. This structural motif can be reproduced by a reaction of trimethylsilyl compounds of methane, halogens, or pse…

Investigation of charge ratio variation in mRNA – DEAE-dextran polyplex delivery systems

2019

Biomaterials 192, 612 - 620 (2019). doi:10.1016/j.biomaterials.2018.10.020

7-Azaindole-fused heterocycles with antitumor activity

2011

Hydrogenolysis of hydroxymatairesinol on Y derived catalysts: a computational study

2010

Hydrogenolysis of 7-hydroxymatairesinol (HMR) to matairesinol (MAT) occurs on palladium supported acidic catalysts. HMR has three stereochemical centres and naturally exists as a mixture of two diastereoisomers, namely RRR-HMR and SRR-HMR. The latter is significantly more reactive than the former, in the reaction above. In order to elucidate the hydrogenolysis mechanism, simple surface events involving HMR derivatives on aluminated faujasite (H-Y) fragments were simulated by quantum chemical calculations. The metallic function of a Pd/H-Y acidic catalyst was also mimicked by a minimal palladium cluster. Stereochemical evidences pointed already out that water β-elimination on the epimeric ce…

Electrical Brain Activity and Its Functional Connectivity in the Physical Execution of Modern Jazz Dance

2020

Besides the pure pleasure of watching a dance performance, dance as a whole-body movement is becoming increasingly popular for health-related interventions. However, the science-based evidence for improvements in health or well-being through dance is still ambiguous and little is known about the underlying neurophysiological mechanisms. This may be partly related to the fact that previous studies mostly examined the neurophysiological effects of imagination and observation of dance rather than the physical execution itself. The objective of this pilot study was to investigate acute effects of a physically executed dance with its different components (recalling the choreography and physical …