5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H- pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist

Bioorganic and Medicinal Chemistry

Volumn 15, Issue 20, 2007, Pages 6556-6564

  Zhang, Puwen ^a   Terefenko, Eugene ^a   Kern, Jeffrey ^a   Fensome, Andrew ^a   Trybulski, Eugene ^a   Unwalla, Ray ^a   Wrobel, Jay ^a   Lockhead, Susan ^a   Zhu, Yuan ^a   Cohen, Jeffrey ^a   LaCava, Margaret ^a   Winneker, Richard C ^a   Zhang, Zhiming ^a  

^a PFIZER INC   (United States)

Author keywords

Non steroidal; PR agonists; PR antagonists; Progesterone receptor (PR)

Indexed keywords

1 CYCLOPENTYL 6 (3,4 DIFLUOROPHENYL) 1,3 DIHYDRO 2H BENZIMIDAZOL 2 ONE; 1 CYCLOPENTYL 6 (3,4 DIFLUOROPHENYL) 1,3 DIHYDRO 2H BENZIMIDAZOLE 2 THIONE; 3 (3 CYCLOBUTYL 2 OXO 2,3 DIHYDRO 1H BENZIMIDAZOL 5 YL) 5 FLUOROBENZONITRILE; 3 (3 CYCLOBUTYL 2 THIOXO 2,3 DIHYDRO 1H BENZIMIDAZOL 5 FLUOROBENZONITRILE; 3 [3 (1 ETHYLPROPYL) 2 OXO 2,3 DIHYDRO 1H BENZIMIDAZOL 5 YL] 5 FLUOROBENZONITRILE; 3 [3 (1 ETHYLPROPYL) 2 THIOXO 2,3 DIHYDRO 1H BENZIMIDAZOL 5 YL] 5 FLUOROBENZONITRILE; 5 (3 CYCLOBUTYL 2 OXO 2,3 DIHYDRO 1H BENZIMIDAZOL 5 YL) 1 METHYL 1H PYRROLE 2 CARBONITRILE; 5 (3 CYCLOBUTYL 2 THIOXO 2,3 DIHYDRO 1H BENZIMIDAZOL 5 YL) 1 METHYL 1H PYRROLE 2 CARBONITRILE; 5 (3 CYCLOPENTYL 2 OXO 2,3 DIHYDRO 1H BENZIMIDAZOL 5 YL) 1 METHYL 1H PYRROLE 2 CARBONITRILE; 5 (3 CYCLOPENTYL 2 THIOXO 2,3 DIHYDRO 1H BENZIMIDAZOL 5 YL) 1 METHYL 1H PYRROLE 2 CARBONITRILE; 5 [3 (1 ETHYLPROPYL) 2 OXO 2,3 DIHYDRO 1H BENZIMIDAZOL 5 YL] 1 METHYL 1H PYRROLE 2 CARBONITRILE; 5 [3 (1 ETHYLPROPYL) 2 THIOXO 2,3 DIHYDRO 1H BENZIMIDAZOL 5 YL] 1 METHYL 1H PYRROLE 2 CARBONITRILE; 6 (3 CHLORO 4 FLUOROPHENYL) 1 (1 ETHYLPROPYL) 1,3 DIHYDRO 2H BENZIMIDAZOL 2 ONE; 6 (3 CHLORO 4 FLUOROPHENYL) 1 (1 ETHYLPROPYL) 1,3 DIHYDRO 2H BENZIMIDAZOLE 2 THIONE; 6 (3 CHLORO 4 FLUOROPHENYL) 1 CYCLOPENTYL 1,3 DIHYDRO 2H BENZIMIDAZOL 2 ONE; 6 (3 CHLORO 4 FLUOROPHENYL) 1 CYCLOPENTYL 1,3 DIHYDRO 2H BENZIMIDAZOLE 2 THIONE; 6 BROMO 1 (1 ETHYLPROPYL) 1,3 DIHYDRO 2H BENZIMIDAZOL 2 ONE; 6 BROMO 1 CYCLOBUTYL 1,3 DIHYDRO 2H BENZIMIDAZOL 2 ONE; 6 BROMO 1 CYCLOPENTYL 1,3 DIHYDRO 2H BENZIMIDAZOL 2 ONE; ALKALINE PHOSPHATASE; ANDROGEN RECEPTOR; COMPLEMENT COMPONENT C3; ETHINYLESTRADIOL; GLUCOCORTICOID; LEVONORGESTREL; MEDROXYPROGESTERONE ACETATE; PROGESTERONE; PROGESTERONE DERIVATIVE; PROGESTERONE RECEPTOR AGONIST; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DECIDUALIZATION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG MECHANISM; DRUG SYNTHESIS; ENZYME ASSAY; FEMALE; HUMAN; HUMAN CELL; MONKEY; NONHUMAN; OVULATION; RAT;

ADMINISTRATION, ORAL; ALKALINE PHOSPHATASE; ANIMALS; CELL LINE, TUMOR; FEMALE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NITRILES; PYRROLES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, PROGESTERONE; STEROIDS;

RATTUS;

EID: 34548185186     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2007.07.011     Document Type: Article

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