SYNTHESIS AND PROGESTERONE-RECEPTOR BINDING-AFFINITY OF SUBSTITUTED 1-PHENYL-7-BENZYL-4,5,6,7-TETRAHYDRO-1H-INDAZOLES

Authors
CONNOLLY PJ WETTER SK BEERS KN HAMEL SC HAYNESJOHNSON D KIDDOE M KRAFT P LAI MT CAMPEN C PALMER S PHILLIPS A
Citation
Pj. Connolly et al., SYNTHESIS AND PROGESTERONE-RECEPTOR BINDING-AFFINITY OF SUBSTITUTED 1-PHENYL-7-BENZYL-4,5,6,7-TETRAHYDRO-1H-INDAZOLES, Bioorganic & medicinal chemistry letters, 7(19), 1997, pp. 2551-2556
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
19
Year of publication
1997
Pages
2551 - 2556
Database
ISI
SICI code
0960-894X(1997)7:19<2551:SAPBOS>2.0.ZU;2-C
Abstract
Research directed toward the discovery of non-steroidal ligands for st eroid receptors led to the preparation of a series of substituted enyl -7-benzyltetrahydroindazole-3-carboxaldehydes. Appropriately substitut ed 3-formyl analogs (4) were found to bind with high affinity to proge sterone 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.