A series of beta-substituted polythiophene derivatives was synthesized through 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).
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Beta-substituted terthiophene [2]rotaxanes.
Chemistry
June 2009
Functional Modules Group, Organic Nanomaterials Center, National Institute for Materials Science, 1-1 Namiki Tsukuba Ibaraki 305-0044, Japan.
Two kinds of beta-substituted terthiophene [2]rotaxanes were synthesized using the host-guest pairs of the electron-deficient cyclophane cyclobis(paraquat-p-phenylene) (CBPQT(4+)) and the electron-rich terthiophenes with diethyleneglycol chains at the beta-position. One is made from the alpha-position non-substituted terthiophene (3 T-beta-Rx) and the other is made from the alpha-dibromo-substituted terthiophene (3 TBr-beta-Rx). The binding constants of the beta-substituted terthiophene threads were confirmed to be smaller than that of the alpha-substituted terthiophene analogue.
View Article and Find Full Text PDFNovel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives.
Bioorg Med Chem Lett
August 1999
Department of Medicinal Chemistry, School of Pharmacy, Purdue University, West Lafayette, IN 47907-1333, USA.
A series of beta-substituted polythiophene derivatives was synthesized through 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).
View Article and Find Full Text PDFRole of conducting polymeric interfaces in promoting biological electron transfer.
Biosens Bioelectron
January 1998
Department of Electronics and Electrical Engineering, University of Glasgow, UK.
In this paper, we explore the role that polymer conductivity and functionality play in determining the nature of molecular recognition at artificial polymer interfaces, as evidenced by electron transfer with the small redox protein, cytochrome c. The relationship is investigated electrochemically using cyclic voltammetry in order to assess the degree of molecular recognition between the biological molecule and carboxyl-functionalized beta-substituted poly(thiophenes) and poly(pyrroles), as well as a co-polymer matrix of these derivatives. In the latter case, the co-polymer film was analysed quantitatively using X-ray photoelectron spectroscopy, and it was found that its composition did not reflect the initial molar ratios of the monomers prior to electrodeposition.
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