Issue 10, 2011
From the journal:

MedChemComm

Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1inhibitors†

Brad E. Sleebs,abc   Alla Levit,abc   Ian P. Street,abc   Hendrik Falk,abc   Tim Hammonds,d   Ai Ching Wong,d   Mark D. Charles,d   Michael F. Olsone  and  Jonathan B. Baell*abc  

* Corresponding authors

a The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria, Australia
E-mail: jbaell@wehi.edu.au.
Tel: +613 9345 2108

b Cancer Therapeutics-CRC P/L, 4 Research Ave, La Trobe R&D Park, Bundoora, Victoria, Australia

c Department of Medical Biology, The University of Melbourne, Parkville, Victoria, Australia

d Cancer Research Technology Ltd, The Cruciform Building, Gower Street London, UK

e The Beatson Institute for Cancer Research, Garscube Estate, Switchback Road, Glasgow, Scotland, UK

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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Article information

DOI
https://doi.org/10.1039/C1MD00137J
Article type
Concise Article
Submitted
26 May 2011
Accepted
12 Jul 2011
First published
12 Aug 2011

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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