Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure.

Abstract:

:New inhibitors have been designed for cdc2 kinase based on a multiple pseudosubstrate structure. The new inhibitors have three different structural components: 3,4-bis(indol-3-yl)maleimide, Ac-Cys-(Ser)-Pro-Lys-Lys-NHMe, and ethyloxy group between the two components. Inhibitory activities toward cdc2 and other protein kinases were investigated, and the compound (21) with Ac-Cys-Pro-Lys-Lys-NHMe connected with the triethylene glycol spacer exhibited the most potent inhibition with relatively high selectivity.

journal_name

Bioorg Med Chem Lett

authors

Sasaki S,Hashimoto T,Obana N,Yasuda H,Uehara Y,Maeda M

doi

10.1016/s0960-894x(98)00163-2

subject

Has Abstract

pub_date

1998-05-05 00:00:00

pages

1019-22

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960894X98001632

journal_volume

8

pub_type

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