Gonadal and stress hormone concentrations of urban European blackbirds

These data describe the levels of certain hormones in faeces and blood of adult urban European blackbirds (Turdus merula) and further conditions associated with the sampling. The samples were collected between March 2011 and May 2013 by Anja Russ, Terézia Lucenicová, Sarah Effertz, Rebecca Thier-Lange, Diana Höhlig, Simon Dietzel, Tobias Köhler, Alexandra Erbach, and Daniela Dunger. The analyses of hormone concentrations were conducted at the Institute of Physiological Chemistry, University of Leipzig, by Susanne Reitemeier, Anne Weissmann, and Jutta Gottschalk. These data have been collected with support of the research project „Birds in illuminated landscapes (BILL)“ funded by the German Federal Ministery of Education and Resarch (BMBF) under the grant: FKZ 033L038E Please note: as decimal marker commas are used

Lead Optimization of 17β-HSD1 Inhibitors of the (Hydroxyphenyl)naphthol Sulfonamide Type for the Treatment of Endometriosis

The reduction of estrone to estradiol, the most potent estrogen in human, is catalyzed by 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1). A promising approach for the treatment of estrogen-dependent diseases is the reduction of intracellular estradiol formation by inhibition of 17β-HSD1. For the species-specific optimization of the (hydroxyphenyl)­naphthols, a combinatorial approach was applied and enhanced by a focused synthesis that resulted in the aromatic-substituted (hydroxyphenyl)­naphthol sulfonamides. Rigidification of <b>12</b> led to the 4-indolylsulfonamide <b>30</b>, which is a highly active and selective human 17β-HSD1 inhibitor, as well as a highly potent and selective inhibitor of 17β-HSD1 from <i>Callithrix jacchus</i>. It shows no affinity to the estrogen receptors α and β and good intracellular activity (T47D). Thus, compound <b>30</b> shows good properties for further ADMET studies and might be a candidate for the in vivo proof of concept in <i>C. jacchus</i>

Overview about the number of detected compounds.

<p>Overview about the number of detected compounds.</p

Number of confirmed compounds retrieved dependent on the adsorbent used.

<p>Number of confirmed compounds retrieved dependent on the adsorbent used.</p

Comparison of TD tube peaks which are in common with the mobile GC-MS and occurring only in TD.

<p>Box-and-whisker plots of the relative peak areas from integration of TD tubes Mix peaks in common with the mobile GC-MS samples (left, Median_common = 4.25 x 10^-4, N_common = 183) and peaks which are unique for TD tubes Mix (right, Median_TD = 0.12 x 10⁻⁴, N_TD = 9217). Bold, solid lines indicate medians, boxes range from the lower to the upper quartiles, lower whiskers are defined as max(min(x), Q_1–1.5 * IQR), upper whiskers equal min(max(x), Q_3 + 1.5 * IQR), open circles are outliers, dotted lines depict the means and asterisk indicates the significant difference. The relative peak areas were log transformed, the y-axis of the plot is on original scale.</p

Compounds in common to TD tubes Mix and mobile GC-MS samples.

<p>Compounds in common to TD tubes Mix and mobile GC-MS samples.</p