Structure-guided design, synthesis, and evaluation of salicylic acid-based inhibitors targeting a selectivity pocket in the active site of human 20α-hydroxysteroid dehydrogenase (AKR1C1)

Journal of Medicinal Chemistry

Volumn 52, Issue 10, 2009, Pages 3259-3264

  El Kabbani, Ossama ^a   Scammells, Peter J ^a   Gosling, Joshua ^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

[No Author keywords available]

Indexed keywords

20ALPHA HYDROXYSTEROID DEHYDROGENASE; 20ALPHA HYDROXYSTEROID DEHYDROGENASE INHIBITOR; 3 BROMO 5 PHENYLSALICYLIC ACID; 3 PHENYL 5 BROMOSALICYLIC ACID; 3,5 DIBROMOSALICYLIC ACID; 3ALPHA HYDROXYSTEROID DEHYDROGENASE; ENZYME INHIBITOR; PHENYL GROUP; SALICYLIC ACID; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG ACTIVITY; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME INHIBITOR INTERACTION; HYDROGEN BOND; HYDROPHOBICITY; IC 50; NONHUMAN; PROGESTERONE METABOLISM; PROTEIN EXPRESSION;

20-HYDROXYSTEROID DEHYDROGENASES; CATALYTIC DOMAIN; CELL LINE; DRUG DESIGN; ENZYME INHIBITORS; HUMANS; HYDROGEN BONDING; PROGESTERONE; PROTEIN BINDING; SALICYLIC ACID; SALICYLIC ACIDS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 66249105304     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm9001633     Document Type: Article

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