Synthesis and progesterone receptor binding affinity of substituted 1-phenyl-7-benzyl-4,5,6,7-tetrahydro-1-indazoles
| Autor: | Kimberly N. Beers, Stephanie C. Hamel, Carolyn Campen, Steven K. Wetter, Stephen S. Palmer, Peter J. Connolly, Pat Kraft, Donna Haynes-Johnson, Audrey Phillips, Margaret Kiddoe, Muh Tsann Lai |
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| Rok vydání: | 1997 |
| Předmět: |
Agonist
Bicyclic molecule Progesterone receptor binding Stereochemistry Chemistry medicine.drug_class medicine.medical_treatment Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis In vitro Steroid In vivo Drug Discovery medicine Molecular Medicine Receptor Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 7:2551-2556 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(97)10016-6 |
| Popis: | Research directed toward the discovery of non-steroidal ligands for steroid receptors led to the preparation of a series of substituted 1-phenyl-7-benzyltetrahydroindazole-3-carboxaldehydes. Appropriately substituted 3-formyl analogs (4) were found to bind with high affinity to progesterone receptors and showed agonist activity in human T47D cells but were inactive in several in vivo models for progestational activity. |
| Databáze: | OpenAIRE |
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