Novel, selective indole-based ECE inhibitors: Lead optimization via solid-phase and classical synthesis
A novel class of indole-based endothelin-converting enzyme (ECE) inhibitors was identified by high throughput screening. We report systematic optimization of this compound class by means of classical and solid-phase chemistry. Optimized compounds with a bisarylamide side chain at the 2-position of the indole skeleton exhibit low-nanomolar activity on ECE.
Brands, Michael,Ergueden, Jens-Kerim,Hashimoto, Kentaro,Heimbach, Dirk,Schroeder, Christian,Siegel, Stephan,Stasch, Johannes-Peter,Weigand, Stefan
p. 4201 - 4205
(2007/10/03)
Synthesis of Novel DNA Binding Agents: Indole-Containing Analogues of Bis-Netropsin
Molecular modelling studies showed that indole dicarboxylic acids are potential linkers for the synthesis of bis-netropsin analogues with a good fit to the minor groove of DNA. To test this hypothesis, 2-carboxyindole-6-acetic acid, indole-2,6-dicarboxyli
Khalaf, Abedawn I.,Pitt, Andrew R.,Suckling, Colin J.,Scobie, Martin,Urwin, John,Waigh, Roger D.,Fishleigh, Robert V.,Young, Stephen C.
p. 751 - 770
(2007/10/03)
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