Tetrahydro-pyrimido-indoles as selective LIMK inhibitors: synthesis, selectivity profiling and structure–activity studies
MEDCHEMCOMM(2016)
Abstract
Extensive structure-activity studies on three different modification sites resulted in a series of LIM kinase inhibitors, containing a novel tricyclic hinge-binding motif based on the pyrrolopyrimidine scaffold. The compounds display a superior selectivity profile and significantly increased on-target activity compared to the former clinical candidate LX7101 (Lexicon Pharmaceuticals). Additionally, a soft drug approach to yield locally active analogues was successfully implemented.
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Key words
selective limk inhibitors,tetrahydro-pyrimido-indoles
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