Issue 10, 2011

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

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

Supplementary files

Article information

Article type
Concise Article
Submitted
26 May 2011
Accepted
18 Jul 2011
First published
12 Aug 2011

Med. Chem. Commun., 2011,2, 982-986

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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