Article
Tri- and tetrasubstituted pyrazole derivates: regioisomerism switches activity from p38MAP kinase to important cancer kinases.
Journal of medicinal chemistry - 26 Jan 2012
Abu Thaher Bassam, Arnsmann Martina, Totzke Frank, Ehlert Jan E, Kubbutat Michael H G, Schächtele Christoph, Zimmermann Markus O, Koch Pierre, Boeckler Frank M, Laufer Stefan A
Abstract excerpt
In the course of searching for new p38α MAP kinase inhibitors, we found that the regioisomeric switch from 3-(4-fluorophenyl)-4-(pyridin-4-yl)-1-(aryl)-1H-pyrazol-5-amine to 4-(4-fluorophenyl)-3-(pyridin-4-yl)-1-(aryl)-1H-pyrazol-5-amine led to an almost complete loss of p38α inhibition, but they...
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