Self-assembly of an anion receptor with metal-dependent kinase inhibition and potent in vitro anti-cancer properties.

One topical area of supramolecular chemistry is the binding of anionic species but despite the importance of anions in diverse cellular processes and for cancer development, anion receptors or 'binders' have received little attention as potential anti-cancer therapeutics. Here we report self-assembling trimetallic cryptands (e.g.

Self-Assembled Anion-Binding Cryptand for the Selective Liquid-Liquid Extraction of Phosphate Anions.

The ligands L and L form trinuclear self-assembled complexes with Cu (i.e. [(L ) Cu ] or [(L ) Cu ] ) both of which act as a host to a variety of anions.

A ligand strand that displays anion-dependant reactivity with acetonitrile; formation of either a mononuclear complex or head-to-tail circular helicate.

The ligand L contains two bidentate domains separated by a 3,3-diamino-2,2'-biphenyl spacer unit and with Cu(ClO) a mononuclear species is formed (e.g. [Cu(L)]).

Self-Assembly of an Anion-Binding Cryptand for the Selective Encapsulation, Sequestration, and Precipitation of Phosphate from Aqueous Systems.

The self-assembled trimetallic species [L Cu ] contains a cavity that acts as a host to many different anions. By using X-ray crystallography, ESI-MS, and UV/Vis spectroscopy we show that these anions are encapsulated both in the solid state and aqueous systems. Upon encapsulation, the anions Br , I , CO , SiF , IO , VO , WO , CrO , SO , AsO , and PO are all precipitated from aqueous solution and can be removed by filtration.

Dihydrogen phosphate-containing dinuclear double assemblies that demonstrate phosphate reactivity to the tetrafluoroborate anion.

The ligands L1 and L2 both form dinuclear assemblies with Cu(ii) and these react with dihydrogen phosphate so that the anion is incorporated within the assembly (e.g. [Cu2L2(H2PO4)]3+).

Ruthenium-Containing Linear Helicates and Mesocates with Tuneable p53-Selective Cytotoxicity in Colorectal Cancer Cells.

The ligands L and L both form separable dinuclear double-stranded helicate and mesocate complexes with Ru . In contrast to clinically approved platinates, the helicate isomer of [Ru (L ) ] was preferentially cytotoxic to isogenic cells (HCT116 p53 ), which lack the critical tumour suppressor gene. The mesocate isomer shows the reverse selectivity, with the achiral isomer being preferentially cytotoxic towards HCT116 p53 .

Structural Strength Benefits Observed at the Hip of Premenarcheal Gymnasts Are Maintained Into Young Adulthood 10 Years After Retirement From the Sport.

Purpose: Premenarcheal female gymnasts have been consistently found to have greater bone mass and structural advantages. However, little is known about whether these structural advantages are maintained after the loading stimulus is removed. Therefore, the purpose of this study was to investigate the structural properties at the hip after long-term retirement from gymnastics.

Catalytic sp -sp Functionalisation of Sulfonamides: Late-Stage Modification of Drug-Like Molecules.

A new application of Pd-catalysed allylation is reported that enables the synthesis of a range of branched sp -functionalised sulfonamides, a compound class for which few reported methods exist. By reacting benzyl sulfonamides with allylic acetates in the presence of Pd catalysts and base at room temperature, direct allylation was efficiently performed, yielding products that are analogues of structural motifs seen in biologically active small molecules. The reaction was performed under mild conditions and could be applied to nanomolar sigma-receptor binders, thus enabling a late-stage functionalisation and efficient expansion of drug-like chemical space.

Formation of a dimer of trinuclear helicates which encapsulates an array of six hydrogen-bonded anions.

The amine-containing ligand L, composed of two bidentate pyridyl-thiazole moieties linked by a 1,3-diaminophenylene unit, reacts with copper(II) ions to form a dinuclear double helicate [Cu2 L2 ](4+) . Reaction of [Cu2 L2 ](4+) with dihydrogen phosphate (0.5 equivalents) gives the unsaturated dinuclear double helicate [Cu2 L2 (OPO3 H2 )](3+) .

Former premenarcheal gymnasts exhibit site-specific skeletal benefits in adulthood after long-term retirement.

Young female gymnasts have greater bone strength compared to controls; although possibly due to selection into gymnastics, it is thought that their loading activity during growth increases their bone mass, influencing both bone geometry and architecture. If such bone mass and geometric adaptations are maintained, this may potentially decrease the risk of osteoporosis and risk of fracture later in life. However, there is limited evidence of the persisting benefit of gymnastic exercise during growth on adult bone geometric parameters.

Higher premenarcheal bone mass in elite gymnasts is maintained into young adulthood after long-term retirement from sport: a 14-year follow-up.

Sports that impact-load the skeleton during childhood and adolescence increase determinants of bone strength such as bone mineral content and density; however, it is unclear if this benefit is maintained after retirement from the sport. The purpose of this study was to assess whether the previously reported higher bone mass in a group of premenarcheal gymnasts was still apparent 10 years after the cessation of participation and withdrawal of the gymnastics loading stimulus. In 1995, 30 gymnasts 8 to 15 years of age were measured and compared with 30 age-matched nongymnasts.

Bone mineral accrual from 8 to 30 years of age: an estimation of peak bone mass.

Bone area (BA) and bone mineral content (BMC) were measured from childhood to young adulthood at the total body (TB), lumbar spine (LS), total hip (TH), and femoral neck (FN). BA and BMC values were expressed as a percentage of young-adult values to determine if and when values reached a plateau. Data were aligned on biological ages [years from peak height velocity (PHV)] to control for maturity.

Effect of maturational timing on bone mineral content accrual from childhood to adulthood: evidence from 15 years of longitudinal data.

A higher bone mass may reduce the risk of osteoporosis and fractures. The role of maturational timing for optimizing bone mass is controversial due to the lack of prospective evidence from childhood to adulthood. The purpose of this study was to examine the long term relationship between the onset of maturation and bone mineral content (BMC) development.

The effect of aquatic exercise and education on lowering fall risk in older adults with hip osteoarthritis.

Objective: To evaluate the effect of aquatic exercise and education on fall risk factors in older adults with hip osteoarthritis (OA).

Method: Seventy-nine adults, 65 years of age or older with hip OA and at least 1 fall risk factor, were randomly assigned to 1 of 3 groups: aquatics and education (AE; aquatic exercise twice a wk with once-a-wk group education), aquatics only (A; 2 wk aquatic exercise) and control (C; usual activity). Balance, falls efficacy, dual-task function, functional performance (chair stands), and walking performance were measured pre- and postintervention or control period.

Does childhood and adolescence fracture influence bone mineral content in young adulthood?

Previous fracture may predispose an individual to bone fragility because of impaired bone mineral accrual. The primary objective of the study was to investigate the influence of fractures sustained during childhood and (or) adolescence on total body (TB), lumbar spine (LS), femoral neck (FN), and total hip (TH) bone mineral content (BMC) in young adulthood. It was hypothesized that there would be lower TB, LS, FN, and TH BMC in participants who had sustained a pediatric fracture.

Assessment of total and central adiposity in Canadian Aboriginal children and their Caucasian peers.

Objective: Although Aboriginal children seem to be more susceptible to developing obesity and metabolic disorders than other ethnic groups in Canada, few studies have examined adiposity comprehensively in this population. The purpose of this study was to assess total and central adiposity in Canadian Aboriginal and Caucasian children matched by age, gender and maturity.

Methods: A total of 212 Aboriginal and 204 Caucasian children (8-17 years) were recruited.

Peak lean tissue mass accrual precedes changes in bone strength indices at the proximal femur during the pubertal growth spurt.

Purpose: We examined the timing of the age and the magnitude of peak lean tissue mass accrual (PLTV) relative to the age and magnitude of two variables of bone strength [peak cross sectional area velocity (PCSAV), and peak section modulus velocity, (PZV)] at the proximal femur in males and females during the adolescent growth spurt. We hypothesized that the age of PLTV would precede the ages of PCSAV and PZV and that there is a positive relationship between the magnitude of PLTV and both PCSAV and PZV in both genders.

Methods: 41 males and 42 females aged 8-18 years were selected from the Saskatchewan Pediatric Bone Mineral Accrual Study (1991-2005).

Does falls-efficacy predict balance performance in older adults with hip osteoarthritis?

This cross-sectional study evaluated the relationship of falls-efficacy to physical performance of functional balance tasks in older adults with hip osteoarthritis (OA). Older adults with hip OA experience several factors associated with fall risk: loss of movement, loss of strength, and increased fear of falls. Seventy-nine men and women age 65 or older were measured for balance, dual task function, and falls-efficacy.

A longitudinal study of the relationship of physical activity to bone mineral accrual from adolescence to young adulthood.

Physical activity in adolescence is beneficial for increasing bone mineral accrual; however, it's unclear whether these benefits persist into adulthood. This prospective study investigated whether physically active adolescents maintained their higher bone mineral content (BMC) into the third decade of life when compared to their less active peers. Data were from 154 subjects (82 females and 72 males) who participated in the University of Saskatchewan's Pediatric Bone Mineral Accrual Study (1991-1997), entry age 8 to 15 years.

The influence of physical activity on lean mass accrual during adolescence: a longitudinal analysis.

During childhood, physical activity is likely the most important modifiable factor for the development of lean mass. However, the effects of normal growth and maturation must be controlled. To distinguish effects of physical activity from normal growth, longitudinal data are required.

The history of falls and the association of the timed up and go test to falls and near-falls in older adults with hip osteoarthritis.

Background: Falling accounts for a significant number of hospital and long-term care admissions in older adults. Many adults with the combination of advancing age and functional decline associated with lower extremity osteoarthritis (OA), are at an even greater risk. The purpose of this study was to describe fall and near-fall history, location, circumstances and injuries from falls in a community-dwelling population of adults over aged 65 with hip OA and to determine the ability of the timed up and go test (TUG) to classify fallers and near-fallers.

Osteoporosis: a pediatric concern?

Osteoporosis and related fractures are a major public health concern globally, and the incidence and subsequent morbidity, mortality and health care costs are expected to increase dramatically over the coming decades. Although osteoporosis was once considered (primarily) a disease of the elderly, there is now universal agreement that the condition has pediatric antecedents. Although genetic factors play an important role in the attainment of an optimal adult (peak) bone mass and strength, lifestyle factors such as physical activity and nutrition are also important determinants of children's bone development.

Do physical maturity and birth date predict talent in male youth ice hockey players?

The aim of this study was to examine the relationships among biological maturity, physical size, relative age (i.e. birth date), and selection into a male Canadian provincial age-banded ice hockey team.

Size-corrected BMD decreases during peak linear growth: implications for fracture incidence during adolescence.

Unlabelled: Peak adolescent fracture incidence at the distal end of the radius coincides with a decline in size-corrected BMD in both boys and girls. Peak gains in bone area preceded peak gains in BMC in a longitudinal sample of boys and girls, supporting the theory that the dissociation between skeletal expansion and skeletal mineralization results in a period of relative bone weakness.

Introduction: The high incidence of fracture in adolescence may be related to a period of relative skeletal fragility resulting from dissociation between bone expansion and bone mineralization during the growing years.