4'-SUBSTITUTED ANALOGS OF IDOXIFENE - ANTIESTROGENS AND CALMODULIN ANTAGONISTS

Authors
HARDCASTLE IR ROWLANDS MG HOUGHTON J JARMAN M
Citation
Ir. Hardcastle et al., 4'-SUBSTITUTED ANALOGS OF IDOXIFENE - ANTIESTROGENS AND CALMODULIN ANTAGONISTS, Bioorganic & medicinal chemistry letters, 5(8), 1995, pp. 805-808
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
8
Year of publication
1995
Pages
805 - 808
Database
ISI
SICI code
0960-894X(1995)5:8<805:4AOI-A>2.0.ZU;2-O
Abstract
4'-substituted analogues of the antiestrogen idoxifene have been prepa red. All the compounds were assayed for antagonism of calmodulin depen dent c-AMP phosphodiesterase and for binding to rat uterine estrogen r eceptor. The 4'-amino compound was the most potent antiestrogen (RBA = 47) whilst retaining a similar calmodulin antagonism to idoxifene.