Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR)

A high throughput screen of Abbott's compound repository revealed that the pyrazolo[3,4-d]pyrimidine class of kinase inhibitors possessed moderate potency for IGF-IR, a promising target for cancer chemotherapy. The synthesis and subsequent optimization of this class of compounds led to the discovery of 14, a compound that possesses in vivo IGF-IR inhibitory activity.     

The Growth of the Shoot Apex of Chenopodium rubrum L. Treated with a Florigenic Extract from Flowering Tobacco Plants: Preliminary Anatomical Observations

Anatomical changes in the shoot apex of Chenopodium rubrum L.treated with an extract from flowering tobacco plants and cultivatedin non-inductive conditions are described. They are comparedwith the anatomy of non-treated vegetative apices and with apicesof plants induced with a short day. Treatment with the extractresulted in both activation of cell division in the upper partof the apex and in apex elongation. Acceleration of leaf primordiainitiation and stimulation of branching took place. The effectcorresponds to the sequence of changes in photoperiodically-inducedplants but is more pronounced. Elongation following 10^–4M GA₃ treatment was of a differentnature; there was only a slight stimulation in the upper partof the apex in contrast with a strong stimulation of growthin length in the lower internodes. These preliminary resultssuggest a similarity between apical changes evoked by a stimulusproduced by short days and an exogenously applied floral stimulus.The changes differed from those caused by exogenous phytohormones. Key words: Chenopodium rubrum, florigen, shoot apex     

Rapamycin analogs with reduced systemic exposure

The synthesis and biological activities of rapamycin (I) analogs modified at the C-40 position are reported. Emphasis placed on compounds that potentially have an improved safety profile on account of their shorter in vivo half-life when compared with rapamycin.     

Comparison of MRI properties between derivatized DTPA and DOTA gadolinium–dendrimer conjugates

In this report we directly compare the in vivo and in vitro MRI properties of gadolinium–dendrimer conjugates of derivatized acyclic diethylenetriamine-N,N′,N′,N″,N″-pentaacetic acid (1B4M-DTPA) and macrocyclic 1,4,7,10-tetraazacyclododecane-N,N′,N″,N?-tetraacetic acid (C-DOTA). The metal–ligand chelates were pre-formed in alcohol prior to conjugation to the generation 4 PAMAM dendrimer (G4D), and the dendrimer-based agents were purified by Sephadex® G-25 column. The analysis and SE-HPLC data indicated chelate to dendrimer ratios of 30:1 and 28:1, respectively. Molar relaxivity measured at pH 7.4, 22 °C, and 3T are comparable (29.5 vs 26.9 mM^?1 s^?1), and both conjugates are equally viable as MRI contrast agents based on the images obtained. The macrocyclic agent however exhibits a faster rate of clearance in vivo (t_1/2 = 16 vs 29 min). Our conclusion is that the macrocyclic-based agent is the more suitable agent for in vivo use for these reasons combined with kinetic inertness associated with the Gd(III) DOTA complex stability properties.     

Simultaneous protease and transglutaminase treatment for shrink resistance of wool

A bioprocess for machine washable wool, combining the advantages of both protease and transglutaminase in a simultaneous enzymatic treatment has been developed. This process reduced the felting tendency of woven wool fabrics by 9% at the expense of only 2% weight and tensile strength loss. In contrast to previously described protease-based processes for shrink resistant wool, the anti-felting properties achieved in the simultaneous enzymatic treatment produced insignificant fibre damage, confirmed also by scanning electron images of the fabrics.     

A new record ofAchlya klebsiana from snakehead,Channa striatus,with fungal infection in Myanmar

This is the first record of the discovery in Myanmar ofAchlya klebsiana, belonging to the family Saprolegniaceae.