Bioorganic and Medicinal Chemistry Letters p. 1019 - 1022 (1998)
Update date:2022-08-05
Topics:
Sasaki, Shigeki
Hashimoto, Tomohiro
Obana, Norihiro
Yasuda, Hideyo
Uehara, Yoshimasa
Maeda, Minoru
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.
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