Structure-based optimization and biological evaluation of human 20α-hydroxysteroid dehydrogenase (AKR1C1) salicylic acid-based inhibitors

European Journal of Medicinal Chemistry

Volumn 45, Issue 11, 2010, Pages 5309-5317

  El Kabbani, Ossama ^a   Scammells, Peter J ^a   Day, Tom ^a   Dhagat, Urmi ^a   Endo, Satoshi ^b   Matsunaga, Toshiyuki ^b   Soda, Midori ^b   Hara, Akira ^b  

^a MONASH UNIVERSITY   (Australia)

^b GIFU PHARMACEUTICAL UNIVERSITY   (Japan)

Author keywords

3 Bromo 5 phenylsalicylic acid; Aldo keto reductase; Cancer; Drug design; Human 20 hydroxysteroid dehydrogenase; Human 3 hydroxysteroid dehydrogenase

Indexed keywords

20ALPHA HYDROXYSTEROID DEHYDROGENASE; 20ALPHA HYDROXYSTEROID DEHYDROGENASE INHIBITOR; 3 BROMO 5 PHENYLSALICYLIC ACID; 3 CHLORO 5 PHENYLSALICYLIC ACID; 3,5 DICHLOROSALICYLIC ACID; 3ALPHA HYDROXYSTEROID DEHYDROGENASE; 4' BUTYL 5 CHLORO 4 HYDROXYBIPHENYL 3 CARBOXYLIC ACID; 4' TERT BUTYL 5 CHLORO 4 HYDROXYBIPHENYL 3 CARBOXYLIC ACID; 5 CHLORO 4 HYDROXY 3' METHYLBIPHENYL 3 CARBOXYLIC ACID; 5 CHLORO 4 HYDROXY 4' ( 1 METHOXYETHYL)BIPHENYL 3 CARBOXYLIC ACID; 5 CHLORO 4 HYDROXY 4' (TRIFLUOROMETHOXY)BIPHENYL 3 CARBOXYLIC ACID; 5 CHLORO 4 HYDROXY 4' ISOBUTYLBIPHENYL 3 CARBOXYLIC ACID; 5 CHLORO 4 HYDROXY 4' METHYLBIPHENYL 3 CARBOXYLIC ACID; 5 CHLORO 4 HYDROXYBIPHENYL 3 CARBOXYLIC ACID; 5 FLUORO 4 HYDROXYBIPHENYL 3 CARBOXYLIC ACID; ALANINE; CARBOXYLIC ACID DERIVATIVE; ENZYME; LEUCINE; OXIDOREDUCTASE INHIBITOR; SALICYLIC ACID; SALICYLIC ACID DERIVATIVE; UNCLASSIFIED DRUG; VALINE;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; COMPLEX FORMATION; CONTROLLED STUDY; DRUG BINDING; DRUG INHIBITION; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; ENZYME METABOLISM; GENE MUTATION; IC 50; NONHUMAN; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; WILD TYPE;

20-HYDROXYSTEROID DEHYDROGENASES; ANIMALS; CATTLE; CELLS, CULTURED; CRYSTALLIZATION; ENZYME INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; KINETICS; MAGNETIC RESONANCE SPECTROSCOPY; MODELS, MOLECULAR; MOLECULAR STRUCTURE; MUTAGENESIS, SITE-DIRECTED; RECOMBINANT PROTEINS; SALICYLIC ACID; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77957854575     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2010.08.052     Document Type: Article

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