165402-16-4Relevant academic research and scientific papers
Aminals in the synthesis of 1,3-substituted propargylamines and 3H-2-vinylidene-3-aminobenzofuran derivatives
Ukhin, L. Yu.,Komissarov, V. N.,Kindeman, S. V.,Khrustalev, V. N.,Struchkov, Yu. T.
, p. 413 - 419 (1994)
Aminals of aromatic o-hydroxyaldehydes react when heated eith terminal acetylenes to form, depending on the reaction conditions and the nature of the starting compounds, 1,3-substituted propargylamines or 3H-2-vinylidene-3-aminobenzofuran derivatives, the
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.
