1227418-60-1Relevant articles and documents
Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potent β-secretase inhibitors
Ghosh, Arun K.,Pandey, Satyendra,Gangarajula, Sudhakar,Kulkarni, Sarang,Xu, Xiaoming,Rao, Kalapala Venkateswara,Huang, Xiangping,Tang, Jordan
, p. 5460 - 5465 (2012/09/25)
Structure-based design, synthesis, and biological evaluation of a series of dihydroquinazoline-derived β-secretase inhibitors incorporating thiazole and pyrazole-derived P2-ligands are described. We have identified inhibitor 4f which has shown potent enzyme inhibitory (Ki = 13 nM) and cellular (IC50 = 21 nM in neuroblastoma cells) assays. A model of 4f was created based upon the X-ray structure of 3a-bound β-secretase. The model suggested possible interactions in the active site.
