Tetracyclic sulfones as potent γ-secretase inhibitors: Synthesis and structure-activity relationship studies

Complex tetracyclic sulfones were designed as gamma-secretase inhibitors and a stereoselective synthesis was achieved. gamma-Secretase activity was seen predominately in the (-) enantiomeric series. Compounds such as 2a and 2b showed remarkable in vitro and in vivo potency. (C) 2010 Elsevier Ltd. All rights reserved.