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


Sleebs, BE; Levit, A; Street, IP; Falk, H; Hammonds, T; Wong, AC; Charles, MD; Olson, MF; Baell, JB
2011-10
MEDCHEMCOMM
Journal Article
2
10
977-981
A high throughput chemical screening campaign has led to the identification of 3-aminobenzo[b]thiophene-2-carboxamides as LIMK I 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 LIMK I inhibitor lead candidate.
ROYAL SOC CHEMISTRY
ACTIN DYNAMICS; KINASE
10.1039/c1md00137j
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Creation Date 2011-10-01 12:00:00