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Tetracyclic sulfones as potent γ-secretase inhibitors: Synthesis and structure–activity relationship studies |
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| Authors: | TK Sasikumar Duane A Burnett Theodros Asberom Wen-Lian Wu Chad Bennett David Cole Ruo Xu William J Greenlee John Clader Lili Zhang Lynn Hyde |
| Institution: | Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA |
| Abstract: | Complex tetracyclic sulfones were designed as γ-secretase inhibitors and a stereoselective synthesis was achieved. γ-Secretase activity was seen predominately in the (?) enantiomeric series. Compounds such as 2a and 2b showed remarkable in vitro and in vivo potency. |
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