Synthesis and progesterone receptor binding affinity of substituted 1-phenyl-7-benzyl-4,5,6,7-tetrahydro-1H-indazoles

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 19, 1997, Pages 2551-2556

  Connolly, Peter J ^a   Wetter, Steven K ^a   Beers, Kimberly N ^a   Hamel, Stephanie C ^a   Haynes Johnson, Donna ^a   Kiddoe, Margaret ^a   Kraft, Pat ^a   Lai, Muh Tsann ^a   Campen, Carolyn ^a   Palmer, Stephen ^a   Phillips, Audrey ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 PHENYL 7 BENZYL 4,5,6,7 TETRAHYDRO 1H INDAZOLE DERIVATIVE; GESTAGEN; PROGESTERONE RECEPTOR; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; BREAST CARCINOMA; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HUMAN; HUMAN CELL; RABBIT; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION; UTERUS;

EID: 0030762285     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)10016-6     Document Type: Article

References (18)

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10. 50 > 1000 nM).
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13. 3H]-R5020 in rabbit uterus progesterone receptor).
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15. 50 range 690-2250 nM), all compounds tested in the antagonist assay were inactive.
16. Not active at the highest concentration tested (10 μM for binding assay, 1 or 3 μM for cell proliferation assay).
17. Compounds were tested orally or as subcutaneous injections in the rabbit endometrial proliferation (Clauberg, C. Zentr. Gynakol. 1930) and rat contragestational assays; certain compounds were also administered directly into the endometrium.
18. 50 = 376 nM).