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Issue 10, 2011
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Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors

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Abstract

A high throughput chemical screening campaign has led to the identification of 3-aminobenzo[b]thiophene-2-carboxamides as LIMK1 inhibitors. Evolution of bicyclic hits to the tricyclic 4-aminobenzothieno[3,2-d]pyrimidine, using a traditional medicinal chemistry SAR guided approach, resulted in a significant increase in potency. Further elaboration has seen the 7-phenyl-4-aminobenzothieno[3,2-d]pyrimidine emerge as a LIMK1 inhibitor lead candidate.

Graphical abstract: Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors

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Publication details

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


Article type: Concise Article
DOI: 10.1039/C1MD00137J
Med. Chem. Commun., 2011,2, 977-981

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    Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors

    B. E. Sleebs, A. Levit, I. P. Street, H. Falk, T. Hammonds, A. C. Wong, M. D. Charles, M. F. Olson and J. B. Baell, Med. Chem. Commun., 2011, 2, 977
    DOI: 10.1039/C1MD00137J

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