Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 16, 2009, Pages 4664-4668

  Washburn, David G ^a   Hoang, Tram H ^a   Frazee, James S ^a   Johnson, Latisha ^a   Hammond, Marlys ^a   Manns, Sharada ^a   Madauss, Kevin P ^a   Williams, Shawn P ^a   Duraiswami, Chaya ^a   Tran, Thuy B ^a   Stewart, Eugene L ^a   Grygielko, Eugene T ^a   Glace, Lindsay E ^a   Trizna, Walter ^a   Nagilla, Rakesh ^a   Bray, Jeffrey D ^a   Thompson, Scott K ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

Agonist; Androgen receptor; Endometriosis; hERG binding; Hormone receptors; Nuclear receptors; OVX rat model; Partial agonist; Progesterone receptor; Progestin

Indexed keywords

2 PYRROLIDONE DERIVATIVE; COMPLEMENT COMPONENT C3; PARTIAL AGONIST; POTASSIUM CHANNEL HERG; PROGESTERONE RECEPTOR; PYRROLIDINE DERIVATIVE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; DOSE RESPONSE; DRUG DESIGN; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SYNTHESIS; ENDOMETRIOSIS; GENE EXPRESSION; HUMAN; HUMAN CELL; IC 50; MAXIMUM PLASMA CONCENTRATION; MONKEY; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BINDING SITES; DRUG DISCOVERY; ETHER-A-GO-GO POTASSIUM CHANNELS; HAPLORHINI; HUMANS; PYRROLIDINONES; RATS; RECEPTORS, PROGESTERONE; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 67651124983     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.06.081     Document Type: Article

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