Synthesis And Progesterone Receptor Binding Affinity Of Substituted 1-Phenyl-7-Benzyl-4,5,6,7-Tetrahydro-1h-Indazoles

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. (C) 1997 Elsevier Science Ltd.