BISINDOLYLMALEIMIDE INHIBITORS OF PROTEIN-KINASE-C - FURTHER CONFORMATIONAL RESTRICTION OF A TERTIARY AMINE SIDE-CHAIN

Authors
DAVIS PD HALLAM TJ HARRIS W HILL CH LAWTON G NIXON JS SMITH JL VESEY DR WILKINSON SE
Citation
Pd. Davis et al., BISINDOLYLMALEIMIDE INHIBITORS OF PROTEIN-KINASE-C - FURTHER CONFORMATIONAL RESTRICTION OF A TERTIARY AMINE SIDE-CHAIN, Bioorganic & medicinal chemistry letters, 4(11), 1994, pp. 1303-1308
Citations number
10
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
11
Year of publication
1994
Pages
1303 - 1308
Database
ISI
SICI code
0960-894X(1994)4:11<1303:BIOP-F>2.0.ZU;2-2
Abstract
A pharmacophore model for the localisation of the cationic binding sit e of bisindolylmaleimide PKC inhibitors is described. This model has b een used to guide selection of further conformationally restricted ter tiary amine analogues, culminating in the identification and synthesis of the potent and highly selective PKC inhibitor, Ro 32-0557.