Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1

Journal of Medicinal Chemistry

Volumn 48, Issue 25, 2005, Pages 8045-8054

  Napper, Andrew D ^a   Hixon, Jeffrey ^a   McDonagh, Thomas ^a   Keavey, Kenneth ^b   Pons, Jean Francois ^b   Barker, Jonathan ^b   Yau, Wei Tsung ^b   Amouzegh, Patricia ^b   Flegg, Adam ^b   Hamelin, Estelle ^b   Thomas, Russell J ^b,d   Kates, Michael ^c   Jones, Stephen ^c   Navia, Manuel A ^a   Saunders, Jeffrey O ^a   DiStefano, Peter S ^a   Curtis, Rory ^a  

^a Elixir Pharmaceuticals Inc   (United States)

^b EVOTEC UK LTD   (United Kingdom)

^c Advanced Synthesis Group   (United States)

^d Siena Biotech SpA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

2 CHLORO 5,6,7,8,9,10 HEXAHYDROCYCLOHEPTA[B]INDOLE 6 CARBOXYLIC ACID AMIDE; 6 CHLORO 2,3,4,9 TETRAHYDRO 1H CARBAZOLE 1 CARBOXAMIDE; ADENOSINE DIPHOSPHATE RIBOSE ACETATE; ENZYME INHIBITOR; INDOLE DERIVATIVE; NICOTINAMIDE; PEPTIDE; SIRTUIN; SIRTUIN 1; SIRTUIN DEACTYLASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CELL MEMBRANE PERMEABILITY; CHO CELL; CONTROLLED STUDY; DEACETYLATION; DRUG BIOAVAILABILITY; DRUG METABOLISM; DRUG SCREENING; DRUG SYNTHESIS; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; IC 50; IN VITRO STUDY; IN VIVO STUDY; MOLECULAR WEIGHT; MOUSE; NONHUMAN;

ANIMALS; BIOLOGICAL AVAILABILITY; CELL MEMBRANE PERMEABILITY; CHO CELLS; CRICETINAE; CRICETULUS; DRUG STABILITY; FLUOROMETRY; HISTONE DEACETYLASES; HUMANS; INDOLES; KINETICS; MICE; MICE, INBRED C57BL; MICROSOMES, LIVER; NAD; NAD+ NUCLEOSIDASE; NIACINAMIDE; RATS; RECOMBINANT PROTEINS; SIRTUINS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 29144501185     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm050522v     Document Type: Article

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