SYNTHESIS OF THE BENZOFURAN ANALOG OF ILV, A NEW-PROTEIN KINASE-C (PKC) ACTIVATOR

Citation
Ap. Kozikowski et al., SYNTHESIS OF THE BENZOFURAN ANALOG OF ILV, A NEW-PROTEIN KINASE-C (PKC) ACTIVATOR, Bioorganic & medicinal chemistry letters, 4(4), 1994, pp. 637-640
Citations number
21
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
4
Issue
4
Year of publication
1994
Pages
637 - 640
Database
ISI
SICI code
0960-894X(1994)4:4<637:SOTBAO>2.0.ZU;2-T
Abstract
In order to probe the effect of small structural changes on the PKC ac tivity of the natural product indolactam V (ILV), a synthesis of its b enzofuran analogue was developed. This compound was found to be simila r in its activity to ILV, exhibiting a Ki of 17.3 +/- 3.7 nM in the di splacement of [H-3]PDBU from PKC alpha.