DESIGN OF NEW INHIBITORS FOR CDC2 KINASE BASED ON A MULTIPLE PSEUDOSUBSTRATE STRUCTURE

Authors
SASAKI S HASHIMOTO T OBANA N YASUDA H UEHARA Y MAEDA A
Citation
S. Sasaki et al., DESIGN OF NEW INHIBITORS FOR CDC2 KINASE BASED ON A MULTIPLE PSEUDOSUBSTRATE STRUCTURE, Bioorganic & medicinal chemistry letters, 8(9), 1998, pp. 1019-1022
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
9
Year of publication
1998
Pages
1019 - 1022
Database
ISI
SICI code
0960-894X(1998)8:9<1019:DONIFC>2.0.ZU;2-H
Abstract
New inhibitors have been designed for cdc2 kinase based on a multiple pseudosubstrate structure. The new inhibitors have three different str uctural components: 3,4-bis(indol-3-yl)maleimide, Ac-Cys-(Ser)-Pro-Lys -Lys-NHMe, and ethyloxy group between the two components. Inhibitory a ctivities toward cdc2 and other protein kinases were investigated, and the compound (21) with Ac-Cys-Pro-Lys-Lys-NHMe connected with the tri ethylene glycol spacer exhibited the most potent inhibition with relat ively high selectivity. (C) 1998 Elsevier Science Ltd. All rights rese rved.