Generating diverse skeletons of small molecules combinatorially

Lack of efficient access to collections of synthetic compounds that have skeletal diversity is a key bottleneck in the small-molecule discovery process. We report a synthesis strategy that involves transforming substrates with different appendages that pre-encode skeletal information, named sigma elements, into products that have different skeletons with the use of common reaction conditions. With this approach, split-pool synthesis can be used to pre-encode skeletal diversity combinatorially and thereby generate such small molecules very efficiently. A split-pool synthesis of more than 1000 compounds produced overlapping, combinatorial matrices of molecular skeletons and appended building blocks in both enantiomeric and diastereomeric forms.     

Discovery of a new gravitational lens system

A new gravitational lens system, the triple radio source MG2016+112, has been discovered. Five emission lines at a redshift of 3.2733+/-0.0014 have been identified in the spectra of two stellar objects of magnitude 22.5 coincident with radio components 3.4 arc seconds apart. The lines are the narrowest ever observed in objects at such a large redshift. The redshift of a 23rd-magnitude extended optical object coincident with the third radio component has not been determined spectroscopically, but its known optical properties are consistent with those of a giant elliptical galaxy with a redshift of about 0.8.     

Infrared Spectroscopy‐Based Metabolomic Analysis for the Detection of Preharvest Sprouting in Grain

Preharvest sprouting of grains causes significant losses to growers and buyers. The problem occurs throughout the world, and economic losses can be millions of dollars. Visual assessment of germination is ineffective because even grains showing no external signs (e.g., having a visible shoot) may still have germinated sufficiently so that it is no longer possible for high‐quality products to be made from them. Current procedures to determine whether a grain has germinated are based around measuring enzyme or starch levels. However, despite protracted efforts to develop enhanced ways to measure germination over the last 50 years, there are currently no sufficiently accurate or reliable approaches available. The present work assesses the potential for infrared spectroscopy‐based metabolomic profiling to assess the germination of barley and wheat. The results indicate that mid‐ and near‐infrared spectroscopy are able to determine if the grain has germinated and give an indication of how long the germination process has been occurring. Both techniques are already well established in the grain industry and have the potential to form the basis of a simple, fast dockside test that would allow segregation of sound and mildly sprouted grain.     

Astrophysics from the moon

The surface of the moon would be an excellent location for astronomical telescopes, and, if a lunar base were to be established, the construction and maintenance of instruments would become feasible. The prospects are reviewed, with particular attention given to large optical aperturesynthesis instruments analogous to the Very Large Array of the National Radio Astronomy Observatory. Typical parameters for a particular system are presented.     

Sodium iodide I 131 treatment of dogs with nonresectable thyroid tumors: 39 cases (1990-2003)

OBJECTIVE: To determine outcome for dogs with nonresectable thyroid carcinomas treated with sodium iodide I 131 and identify factors associated with outcome. DESIGN: Retrospective case series. Animals-39 dogs. PROCEDURES: A definitive or presumptive diagnosis of thyroid tumor was made on the basis of cytologic or histologic examination, abnormal accumulation of sodium pertechnetate Tc 99m during scintigraphy, or both, and dogs were treated with sodium iodide I 131. Dogs with cervical thyroid tumors were evaluated 3 to 6 weeks after 131I therapy, and residual tumor was resected when feasible. RESULTS: Prior to 131I therapy, 32 dogs had a solitary mass and 7 had metastases; 21 were hyperthyroid, 16 were euthyroid, and 2 were hypothyroid. Median survival time for dogs with local or regional tumors (ie, stage II or III) was significantly longer (839 days) than median survival time for dogs with metastasis (366 days). Tumor site (cervical vs ectopic), dose of sodium iodide I 131, age, body weight, treatment (131I therapy alone vs 131I therapy followed by surgery), and serum T4 concentration prior to 131I therapy were not significantly associated with survival time. Three dogs died of radioiodine-associated myelosuppression within 3 months after treatment, but no specific factor associated with development of toxicosis was identified. CONCLUSIONS AND CLINICAL RELEVANCE: Results suggested that 131I therapy may result in prolonged survival times in dogs with nonresectable thyroid tumors, regardless of serum thyroxine concentration prior to treatment. Dogs undergoing 131I therapy should be monitored for signs of bone marrow suppression.