10468-23-2Relevant academic research and scientific papers
The hit-to-lead optimization of 1,2,3,4,4a,9a-hexahydro-1H-xanthenes as glucocorticoid receptor antagonists
Zhu, Yan-Hui,Zhang, Meng,Li, Qun-Yi,Liu, Qing,Zhang, Jie,Yuan, Yun-Yun,Nan, Fa-Jun,Wang, Ming-Wei
supporting information, p. 693 - 698 (2014/06/09)
The structure-activity relationship (SAR) study of a 1,2,3,4,4a,9a- hexahydro-1H-xanthene series of selective, human glucocorticoid receptor α (hGRα) antagonists is reported. Compounds were screened using hydroxyapatite-based GR binding and MMTV-Luc co-transfection reporter gene assays. Four different regions of the scaffold were modified to assess the effects on hGRα antagonism and related potency. Compound 8d exhibits an 8-fold better bioactivity than the original hit 1a, as well as an improved chemical stability, which make it a promising lead for the subsequent optimization.
On the Electrochemical Oxidation of Enamines
Schoeller, Wolfgang W.,Niemann, Juergen,Rademacher, Paul
, p. 369 - 374 (2007/10/02)
The electrochemical properties of enamines of the cyclic ketones cyclo-pentanone, -hexanone, -heptanone, and -octanone with the cyclic amines pyrrolidine, piperidine, 1-methylpiperazine (1-MP), morpholine (MO), hexa-, and hepta-methyleneimine are investigated with the aid of cyclic voltammetry.The oxidations are totally irreversible.The lifetime of the intermediate cation radicals are shorter than 0.2 ms as determined by double potential step chronoamperometry.The anodic peak potentials depend on the amine component in the order of ring sizes 57; 861-MPMO.The variation of the ketone component shows no significant influence on the peak potentials.The ionization potentials of the enamines were measured and correlated with the anodic peak potentials.
