Polymer-supported <i>N</i>-Methylmorpholine <i>N</i>-Oxide as an efficient and readily recyclable co-oxidant in the TPAP oxidation of alcohols

A readily available, polymer supported amine N-oxide has been prepared and shown to be a practicable, efficient, selective, and readily recyclable co-oxidant in the TPAP oxidation of alcohols

High loading polymer-supported <i>N</i>-Methylmorpholine <i>N</i>-Oxide; a practically efficient and readily recyclable promoter of the Pauson-Khand reaction

A high loading polymer supported amine N-oxide has been prepared and shown to be a good, practicable, and readily recyclable promoter of the Pauson-Khand reaction under mild conditions, generally affording excellent yields of cyclopentenones. In addition, use of N-phenylsulfonyl oxaziridine as a co-oxidant allows use of reduced quantities of the readily available parent polymer-supported amine without the need for prior oxidation of the resin

Spring phytoplankton onset after the ice break-up and sea-ice signature (Adélie Land, East Antarctica)

The phytoplankton onset following the spring ice break-up in Adélie Land, East Antarctica, was studied along a short transect, from 400 m off the continent to 5 km offshore, during the austral summer of 2002. Eight days after the ice break-up, some large colonial and solitary diatom cells, known to be associated with land-fast ice and present in downward fluxes, were unable to adapt in ice-free waters, while some other solitary and short-colony forming taxa (e.g., Fragilariopsis curta, F. cylindrus) did develop. Pelagic species were becoming more abundant offshore, replacing the typical sympagic (ice-associated) taxa. Archaeomonad cysts, usually associated with sea ice, were recorded in the surface waters nearshore. Rough weather restricted the data set, but we were able to confirm that some microalgae may be reliable sea-ice indicators and that seeding by sea ice only concerns a few taxa in this coastal area of East Antarctica. Keywords: Ice break-up; phytoplankton; sea-ice signature; East Antarctica (Published: 10 January 2011) Citation: Polar Research 2011, 30, 5910, doi: 10.3402/polar.v30i0.591

Identification and optimization of a novel series of selective PIP5K inhibitors

Phosphatidyl inositol (4,5)-bisphosphate (PI(4,5)P 2) plays several key roles in human biology and the lipid kinase that produces PI(4,5)P 2, PIP5K, has been hypothesized to provide a potential therapeutic target of interest in the treatment of cancers. To better understand and explore the role of PIP5K in human cancers there remains an urgent need for potent and specific PIP5K inhibitor molecules. Following a high throughput screen of the AstraZeneca collection, a novel, moderately potent and selective inhibitor of PIP5K, 1, was discovered. Detailed exploration of the SAR for this novel scaffold resulted in the considerable optimization of both potency for PIP5K, and selectivity over the closely related kinase PI3Kα, as well as identifying several opportunities for the continued optimization of drug-like properties. As a result, several high quality in vitro tool compounds were identified (8, 20 and 25) that demonstrate the desired biochemical and cellular profiles required to aid better understanding of this complex area of biology. </p