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Issue 3, 2016
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Tetrahydro-pyrimido-indoles as selective LIMK inhibitors: synthesis, selectivity profiling and structure–activity studies

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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.

Graphical abstract: Tetrahydro-pyrimido-indoles as selective LIMK inhibitors: synthesis, selectivity profiling and structure–activity studies

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Publication details

The article was received on 14 Oct 2015, accepted on 07 Dec 2015 and first published on 10 Dec 2015


Article type: Research Article
DOI: 10.1039/C5MD00473J
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Med. Chem. Commun., 2016,7, 478-483

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    Tetrahydro-pyrimido-indoles as selective LIMK inhibitors: synthesis, selectivity profiling and structure–activity studies

    J. Alen, A. Bourin, S. Boland, J. Geraets, P. Schroeders and O. Defert, Med. Chem. Commun., 2016, 7, 478
    DOI: 10.1039/C5MD00473J

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