SYNTHESIS AND BIOLOGICAL EVALUATION OF CONFORMATIONALLY CONSTRAINED BICYCLIC AND TRICYCLIC BALANOL ANALOGS AS INHIBITORS OF PROTEIN-KINASE-C

Authors
MENDOZA JS JAGDMANN GE GOSNELL PA
Citation
Js. Mendoza et al., SYNTHESIS AND BIOLOGICAL EVALUATION OF CONFORMATIONALLY CONSTRAINED BICYCLIC AND TRICYCLIC BALANOL ANALOGS AS INHIBITORS OF PROTEIN-KINASE-C, Bioorganic & medicinal chemistry letters, 5(19), 1995, pp. 2211-2216
Citations number
17
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
19
Year of publication
1995
Pages
2211 - 2216
Database
ISI
SICI code
0960-894X(1995)5:19<2211:SABEOC>2.0.ZU;2-A
Abstract
A series of conformationally constrained bicyclic (20-25 and 28) and t ricyclic (26 and 27) balanol analogues was prepared and evaluated as i nhibitors of protein kinase C (PKC). Of special interest are bicyclic balanol analogues 20 and 24 and the tricyclic analogue 26, which not o nly retain the nanomolar activity for most PKC isozymes, but also disp lay good selectivity over c-AMP dependent protein kinase (PKA).