Study of E/Z isomerization in a series of novel non-ligand binding pocket androgen receptor antagonists

We report the conformational analysis of a series of 3-hydroxy-N′- ((naphthalen-2-yl)methylene)naphthalene-2-carbohydrazides. This class of compounds has recently been reported as androgen receptor (AR)-coactivator disruptors for potential application in prostate cancer therapy. Definition of the E/Z isomerism around the imine linker group (hydrazide) is significant from a mechanistic point of view. A detailed study using theoretical calculations coupled with experimental techniques has allowed us determine an initial preference for the E isomer. The biological activity of newly synthesized compounds at the androgen receptor, along with a series of structural analogs, was determined and provides the basis for preliminary qualitative structure-activity relationship analysis. © 2012 American Chemical Society.Peer Reviewe

Solar Ultraviolet Exposures At Ground Level In Tree Shade During Summer In South East Queensland

Data are presented on the effect of the tree canopy transmittance in the visible waveband (VT), canopy width, height and height of the start of the tree canopy (CH) on the solar UV in tree shade on a horizontal plane at ground level during a Southern Hemisphere summer. Of these factors, the VT and CH have an influence on the UV irradiances in the tree shade. The shade ratios (UV in tree shade to that in full sun) for erythemal UV ranged from 0.71 to 0.42, 0.54 to 0.29 and 0.63 to 0.41 for morning, noon and afternoon, respectively, for the VT range of 0.4-1.0. Over the same VT range, the shade ratios for UVA ranged from 0.61 to 0.28, 0.50 to 0.22 and 0.49 to 0.29 for morning, noon and afternoon, respectively. The UV exposures in the tree shade decreased with the VT with a marginally higher decrease in the irradiances for the UVA compared to the erythemal UV. Despite the protection by the tree shade, significant UV in the tree shade of approximately 4 MED (minimum erythemal dose) were received for the latitude in this research on a cloud free summer day on a horizontal plane over a 2-h period centred about solar noon