Probing the binding pocket of the active site of aromatase with 6-ether or 6-ester substituted androst-4-ene-3,17-diones and their diene and triene analogs

Steroids

Volumn 65, Issue 12, 2000, Pages 871-882

  Numazawa, Mitsuteru ^a   Shelangouski, Momoko ^a   Nagasaka, Mina ^a  

^a TOHOKU PHARMACEUTICAL UNIVERSITY   (Japan)

Author keywords

6 ester substituted C19 steroid; 6 ether substituted C19 steroid; Aromatase inhibitor; Molecular modeling; Structure activity relationship; Time dependent inactivation

Indexed keywords

6 ACETOXYANDROST 4 ENE 3,17 DIONE; 6 ETHOXYANDROST 4 ENE 3,17 DIONE; 6 HEXAOXYANDROST 4 ENE 3,17 DIONE; 6 METHOXYANDROST 4 ENE 3,17 DIONE; ANDROSTENEDIONE; AROMATASE INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; COMPETITIVE INHIBITION; ENZYME ACTIVE SITE; ENZYME BINDING; ENZYME INACTIVATION; ENZYME INHIBITION; ESTERIFICATION; HYDROPHOBICITY; MOLECULAR MODEL; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

ANDROSTENEDIONE; ANTINEOPLASTIC AGENTS; AROMATASE; AROMATASE INHIBITORS; BINDING SITES; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTROSTATICS; ENZYME ACTIVATION; ENZYME INHIBITORS; ESTERS; ETHERS; HUMANS; KINETICS; MICROSOMES; MODELS, MOLECULAR; PLACENTA; PROTEIN BINDING; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY; TIME FACTORS;

EID: 0033758790     PISSN: 0039128X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0039-128X(00)00169-0     Document Type: Article

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