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Issue 10, 2011
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Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors

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Abstract

7-Phenyl-4-aminobenzothieno[3,2-d]pyrimidines were previously reported to exhibit moderate LIMK1 inhibition. Further exploration of SAR around the 7-phenyl moiety has led to the development of a lead series with an increased potency for LIMK1. Evaluation of physicochemical and ADME properties, and off-target kinase screens has seen this novel series emerge as a promising platform for a set of tool compounds for evaluating LIMK as a therapeutic target.

Graphical abstract: Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors

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Publication details

The article was received on 26 May 2011, accepted on 18 Jul 2011 and first published on 12 Aug 2011


Article type: Concise Article
DOI: 10.1039/C1MD00138H
Med. Chem. Commun., 2011,2, 982-986

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    Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors

    B. E. Sleebs, D. Ganame, A. Levit, I. P. Street, A. Gregg, H. Falk and J. B. Baell, Med. Chem. Commun., 2011, 2, 982
    DOI: 10.1039/C1MD00138H

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