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

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      Publication Details (including relevant citation   information):

      Medicinal   Chemistry Communications (2011),   2,   977-981


      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.

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