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Bioorg Med Chem Lett. 2008 Jul 15;18(14):4232-6. doi: 10.1016/j.bmcl.2008.05.064. Epub 2008 May 20.

Discovery of a novel series of Notch-sparing gamma-secretase inhibitors.

Author information

1
Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA. krefta@wyeth.com

Abstract

Using a cell-based assay, we have identified a new series of Notch-sparing gamma-secretase inhibitors from HTS screening leads 2a and 2e. Lead optimization studies led to the discovery of analog 8e with improved gamma-secretase inhibitory potency and Notch-sparing selectivity.

PMID:
18556202
DOI:
10.1016/j.bmcl.2008.05.064
[Indexed for MEDLINE]

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