Three new abietane-type diterpenoids, 7a-butoxyabieta-8,12-diene-11,14-dione (1), 6a,7a-dihydroxyabieta-8,12-dien-11,14-dione (2), and 6a,7b-dihydroxyabieta8,12-diene-11,14-dione (3) were isolated from the bark of Cryptomeria japonica D. Don. Their structures were established by means of 1D and 2D NMR, IR, UV, and HR-EI-MS spectra and comparison with the data of known analogues. ã 2016 Publishe...

Insulin-like growth factor-1 receptor (IGF-1R) is a growth factor receptor tyrosine kinase acting as a critical mediator of cell proliferation and survival. Novel 5-benzylidenethiazolidine-2,4-dione (5) and 5-(furan-2-ylmethylene)thiazolidine-2,4-dione (6) compounds were identified as potent and selective IGF-1R inhibitors via hierarchical virtual screening. Initial SAR and biological activity ...

The pharmacokinetics and metabolism of linagliptin (BI1356, 8-(3R-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione) were investigated in healthy volunteers. The 10- and 5-mg (14)C-labeled drug was administered orally or intravenously, respectively. Fecal excretion was the dominant excretion pathway with 84.7% (p.o.) and 58.2% (i.v.) of ...

This paper describes the properties and partial purification from Pseudomonas testosteroni of enzymes concerned with the introduction of unsaturation into ring A of 3-ketosteroids. These enzymes promote the formation of the A1e4-diene-3-one structure from steroids bearing C-19 angular methyl groups and the formation of ring A phenols from lQ-nor-steroids. P. testosteroni is a strict aerobe whic...