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

Brad Sleebs, Alla Levit, Ian Philip Street, Hendrik Falk, Timothy R Hammonds, Ai Ching Wong, Mark D Charles, Michael F Olson, Jonathan Bayldon Baell

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)977 - 981
Number of pages5
JournalMedChemComm
Volume2
Issue number10
DOIs
Publication statusPublished - 2011
Externally publishedYes

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