Design and synthesis of tricyclic sulfones as γ-secretase inhibitors with greatly reduced Notch toxicity

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 8, 2010, Pages 2591-2596

  Xu, Ruo ^a   Cole, David ^a   Asberom, Ted ^a   Bara, Tom ^a   Bennett, Chad ^a   Burnett, Duane A ^a   Clader, John ^a   Domalski, Martin ^a   Greenlee, William ^a   Hyde, Lynn ^a   Josien, Hubert ^a   Li, Hongmei ^a   McBriar, Mark ^a   McKittrick, Brian ^a   McPhail, Andrew T ^b   Pissarnitski, Dmitri ^a   Qiang, Li ^a   Rajagopalan, Murali ^a   Sasikumar, Thavalakulamgar ^a   Su, Jing ^a   Tang, Haiqun ^a   Wu, Wen Lian ^a   Zhang, Lili ^a   Zhao, Zhiqiang ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

^b DUKE UNIVERSITY   (United States)

Author keywords

Secretase inhibitor; Alzheimer's disease; CYP; Notch toxicity

Indexed keywords

GAMMA SECRETASE INHIBITOR; NOTCH RECEPTOR; SULFONE DERIVATIVE;

ANIMAL EXPERIMENT; ARTICLE; DRUG ACTIVITY; DRUG DESIGN; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; MOUSE; NONHUMAN;

AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; MICE; MODELS, MOLECULAR; RECEPTORS, NOTCH; SULFONES;

EID: 77950028986     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.02.080     Document Type: Article

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