Novel protein kinase C inhibitors: Synthesis and PKC inhibition of beta-substituted polythiophene derivatives

Authors
Xu, WC Zhou, Q Ashendel, CL Chang, CT Chang, CJ
Citation
Wc. Xu et al., Novel protein kinase C inhibitors: Synthesis and PKC inhibition of beta-substituted polythiophene derivatives, BIOORG MED, 9(15), 1999, pp. 2279-2282
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
15
Year of publication
1999
Pages
2279 - 2282
Database
ISI
SICI code
0960-894X(19990802)9:15<2279:NPKCIS>2.0.ZU;2-4
Abstract
A series of beta-substituted polythiophene derivatives was synthesized thro ugh palladium-catalyzed coupling reaction. Their structure-protein kinase C (PKC) inhibitory activity relationship was studied. The carboxaldehyde and hydroxymethyl derivatives of alpha-terthiophene were potent PKC inhibitors (IC50 = 10(-7) M). (C) 1999 Elsevier Science Ltd. All rights reserved.